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About the Book

This book is prepared to facilitate the studying Pharmacology for students of any medical field
(Pharmacy , Medicine , Dentistry, Nursing, etc.)

As Pharmacology contain too many drugs that are hard to be memorized even if you are
planning to take a Pharmacology exam or you are studying pharmacology for any purpose , This
book will facilitate your mission .

This book is only about 40 pages that make Pharmacology study easy as drinking a cup of
water .

Pharmacology Mind maps


By Raafat Gergis
st
1 Edition ,
All Right are reserved for the Author
Copyright© 2016 Raafat Gergis
Navigate to Contents
Drugs for Bronchial Asthma
Drugs for cough
Drugs for Peptic ulcer
GIT drugs
Sedatives and hypnotics
General Anesthesia
Local Anesthesia
Opioid analgesics
Anti-Psychotic Drugs
Anti-Depressants Drugs
ANTI-EPILEPTIC DRUGS
ANTI-MIGRINE DRUG
P H R M A C O L O G Y - NOTE 1 - Treatment of Asthma

Drugs for Asthma

Anti-inflammatory
Bronchodilators Anti-leukotrienes Mast cell stabilizers
(glucorticosteroids)

β2-adrenergic LT synthesis LT receptor Sodium


Methylxanthines Anti-muscarinic Beclomethasone inhibitor antagonist Cromoglycate
agonist

Salbutamole Theophylline Ipratropium Hydrocortisone Zileuton Montelukast

Terbutaline Aminophylline Prednisolone Mucosal Mucosal


inflammation edema

Salmaterol Broncho- Mucus


constriction secretion
Role of
Leukotrines
in asthma

•Contraction of airway smooth muscle.


Clinical features of bronchial

•leadiŶg to acute dyspnea & airway Uses of bronchodilator


obstruction.
•Mucus hypersecretion.
•leadiŶg to mucus pulgging.
•Airway inflamation. for acute during acute for quick
. broncho- phase of reduce airway
asthma.

•leadiŶg to bronchodema
spasm asthma attack constriction
P H R M A C O L O G Y - NOTE 1 - Treatment of Asthma

 Bronchodilaters
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Salbutamole Fast onest. Given inhaler or Nebulizer. Bind to β-receptor & stimulate Used for acute attack. Tremor.
adrenergi

Terbutaline Short duration. Less side effect. adenylcyclase. Vascular headache.


Β2-

Given orally, S.C, IV or IM.  Leading to  cAMP.


Salmaterol Slow onest. Used for long term therapy.
Large dose.  Bronchodilatation.
Long duration.
More side effect.
Theophylline Has narrow theraputic index. Inhibit PDEI. GIT: nausea, vomiting .
Given orally.  Leading to  cAMP. CNS: stimulation insomnia,
Cause GI irritant. Ca++ influx irritabillity & headach.
Methylxanthines

Bronchodilatation CVS:  BP, arrhythmia.


Water mixture of Theophylline + Ethylenediamine. 1) CNS stimulation. Kidney: diuresis.
Aminophylline
2) Cardiac muscle stimulation.
Given orally, rectally (suppositories) or injection.
3) Diuresis.
4) S.M. relaxtion of bronchial & uterus.
5) Periphral & cornory vasodilatation.
6) Cerebralvasoconstriction.
Anti- Ipratropium It is poorly absobed from the GIT. Blocking M receptor in bronchial Dry mouth.
musc  So,it given by inhalation. smooth muscle.
rinic
Slower onest & longer duration than salbutamol.  Bronchodilatation

 Anti-inflammatory(Glucorticosteroid)
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Beclomethasone Given by inhalation, orally or IV. 1) Reduce mucosal edema. If taken by inhalation,
2) Sensitize β2-agonist. Dysphonia (hoarseness).
Hydrocortisone 3) Reduce inflammatory cell activation Oral candidiasis (fungal
Prednisolone infection).
 Anti-Leukotrienes
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Zileuton  1) Inhibit lipoxygenase enzyme. To prevent asthma caused by 
2) Reduce conversion of AA to LT.  Aspirin.
So, it is …  NASID.
 Broncodilater.
 Anti-inflammatory.
Montelukast  1) Blocking LT receptors. To prevent asthma caused by 
2) Inhibit bronchoconstriction caused by LT  NASID & Exercise.
Mast Cell Stabilizers

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Na Cromoglycate Given by inhalation. Reduce the mediators that release Prophylaxis aginst asthma Cough.
from mast cell in response to allergen attack. Wheeze.
Ketotifen Given orally.
that cause bronchoconstriction.
P H R M A C O L O G Y - NOTE 1 - Treatment of Cough
It clears the excess secretions
& inhaled foreign matters.
Productive Cough Expectorants are used.

Common causes of Cough: Dry cough has no useful


Non-Productive function.
• 1) Acute Respiratory Infection. Cough Anti-tussives are used.

• Upper respiratory infection.


• Pneumonia.
• Bronchitis
• They should be used for dry cough.
• 2) Chronic Respiratory Infection. • because it suppress cough reflex, it should not be used in
• TB. Anti-tussive the presence of bronchial secretions.
• Postnasal drip.
• 3) Airway Diseases.
• It reduces the sensitivity of periphral cough receptors to it's
• Asthma. Locally anti- activators which include irritants & autacoids (Bradykinine).
• COPD. tussive
• 4) Irritants.
• Cigarettes smoking. • They clear airway from mucus secretion by:
• ability to expectorate sputum.
• Inhaled foreign bodies. Mucoactive
Agents • 
mucus hyper secretion.
• 5) Drug Induced.
• Inhaled drugs (aerosols).
• ACE-inhibitors (anti-hypertensive).

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P H R M A C O L O G Y - NOTE 1 - Treatment of Cough
DRUDS FOR COUGH

Anti-tussives Mucoactive
Drugs Agents

Centrally Peripherally Expectorants Mucolytics

Opioid Hyperosmolar Classic


Dervatives Anti-histamins Above Larynx Below Larynx Na citrate mucolytic
saline

Diphenhydram steam with or without Na


Codeine K citrate NAS
ine Lozenge (menthol & benzoin bicarbonate
tincture)

Ammonium Peptide
Pholcodeine Syrup mucolytic
Nebulized Cloride Na Iodide
Lignocaine

Dextrome-
K Iodide Guaifenesin Dornasealpha
thorphan Nebulized
Benzocaine

Noscapine Creosote Guaicolate others

Centrally & Bromhexine


Periphrally

Benzonatate Ambroxol

Mucoregulatory

Anti- Macrolide Anti-


cholinergic Antibiotics inflammatory

Ipratropium Azithromycin Indomethacin Corticosteroids

Atropine

|
P H R M A C O L O G Y - NOTE 1 - Treatment of Cough

 Anti-Tussives (cough suppressent)


DRUGS PHARMACOKINETIC ACTION & ITS MECHANISM USES SIDE EFFECT
Codeine They suppress cough reflex by Nausea.
Pholcode Derict inhibition of Cough Center in the Dizziness.
Dervative
Opioid

medulla.
Acting Centarlly

Dextromethorphan Urenary retention.


Constipation.(vi)
Noscapine
Diphenhydramine It depresses CNS including Cough Center. Sedation.
Histamine

Drowsiness.
Anti-

Dizziness.

Lozenges They are demulcents. They form gelatious coat that protects the Used for cough of
Above
Larynx

Syrup(honey)
inflammed skin  Sore throat.
 Pharyngitis.
Acting Periphrally

Steam Without tooking, Taken with or Promote secretion of dilute mucus,


it taken by without (menthol  To protect inflammed mucosa
& benzoin
inhalation .
tincture)
Larynx
Below

NebulizedLigocaine 1) Local anesthesia. During fiber optic bronchoscopy.


2) Blooking mucosal cough receptors. intractable cough in bronchial carcinoma.
Nebulized
Benzocaine
Acting both Benzonatate Chemichally, it is related to 1) In lungs, acting on
Centrally tetracaine (local ansthesia). Stretch & cough receptors.
&Periphrally 2) Act on CNS
 Mucoactive Agents (Expectorants)
o They volume or hydration of airway secretion.
o They improve expectoration of respiratory mucus secretion.
DRUGS PHARMACOKINETIC ACTION & ITS MECHANISM USES SIDE EFFECT
Hyperosmolar Saline (10 ml of 6% saline). Used in fibross & bronchiectasis.
Inhaled by ultrasonic nebulisation.
Na citrate 1) Stimulate secretion of low viscosity watery Used in early dry stage of acute bronchitis.
K citrate mucus & sissolve it.
To make it thinner less sticky.
Na bicarbonate
2) elasticity of bronchi.
To easily expectorate the mucus.
Expectorants

Ammonium Cloride Stimulate secretion of low viscosity watery mucus


By stimulation of sensory nerve ending in
the stomach.
Na Iodide 1)Stimulate secretion of low viscosity watery mucus Chronic respiratory disease.
K Iodide 2)has mucolytic action. Chronic asthma.
Guaifenesin 1)respiratorysecretion.
2)adhesiveness & surface tension of viscid sputum
Creosote 1)sputum. Lung absess.
2)has mild antiseptic & deodrant action. Chronic bronchitis.
Guaicolate Bronchiectasis.

|
P H R M A C O L O G Y - NOTE 1 - Treatment of Cough

 Muocoactive Agentgs (Mucolytic)


o They 
viscosity & of elasticity airway secretion & 
mucociliary & cough clearance.
DRUGS PHARMACOKINETIC ACTION & ITS MECHANISM USES SIDE EFFECT
N-acetulcysteine (NAC) Taken orally or by inhalation. 1) Hydrolyse disulfid bond of mucin. In condition associated with viscous mucus Bronchospasm.
It is a precursor of intracellular
cysteine & glutathione.
So, mucus loss it’s viscosity & elasticity. secretion:
Chronic bronchitis, emphysema,
 Prevent by
β2-agonist.
2) Act as antioxidant.
brochiectasis & cystic fibrosis. Disagreeable odor.
So, it prevent pulmonary injury in patient (ARD): bronchitis, pneumonia & asthma.  Sulfur odor &
Classic Mucolytic

with COPD or lung cancer. Post-operative & post-traumatic taste.


pulmonary complications. GI irritation.
Care of tracheostomy. Nausea.
Act as antidote for paracetamol overdose. Vomiting.
Stomatitis.
Dornase alpha Taken by nebulisation. For cystic fibrosis. Allergicreaction.
Mucolytic

Pharyngitis.
Peptide

Laryngitis.
Voice alteration.

Bromhexine It is an expectorant & mucolytic 1) Liquefy mucus. Acute bronchitis. Rhinorrhea.


drug.
Taken orally, parentral or by
 By viscosity of bronchial secretion. Chronic bronchitits.
COPD.
Lacrimation.
Gastric irritant.
2) Enhance expectoration.
inhalation.  Avoid with

Others

Ambroxol Taken orally. By the rate of microciliary. antacid.


has less GI irritant.
 Mucoactive Agents (Mucoregulatory Agents)
o They 
airway mucus hyper secretion which caused by goblet cells & submucosal gland.
DRUGS PHARMACOKINETIC ACTION & ITS MECHANISM USES SIDE EFFECT
Indomethacine inflammation which leading to mucus hyper Panbronchiolits
nflammatory

secretion.
Anti-i

Corticosteroid

Ipratropium mucus volume that secreted in chronic


bronchitis.
Anticholinergic

Atropine mucus hypersecrtion. used pre-anesthetically for endotracheal


intubation.

Azithromycin Taken orally for long term


Macrolide
antibiotics

administion.

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P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer

DRUGS FOR PEPTIC ULCER

Drugs Affecting Mucosal Drugs erdicate


HCL Protictive Agents H. Pylori

Colloidal Bismuth Quadruple


Antacids H2 Blocker Sucralfate Misoprostol
Triple Therapy Therapy
compounds

Bismuth Omeprazole OR Omeprazole OR


AL(OH)3 Cimetidine Lansoprazole Lansoprazole
Subsalycilate (PPI) (PPI)

Bismuth
Mg(OH)2 Ranitidine Bismuth
Sobcitrate Clarithromycin
Subsalycilate

Amoxycillin OR
Famotidine Metronidazole
Metronidazole

Proton Pump
Anti-muscarinic Tetracycline
Inhibitors

Omeprazole Pirenzepine

• It is caused by imbalance between:


(GU & DU)
Peptic Ulcer

• Protective Factors
Lansoprazole • (Mucus & Bicharbonate).
• Dameging Factors
• (HCL & pepsin).
• So, it is caused by either 
DF or PF.
P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer
 Drugs Affecting Gastric (HCL) Acid
DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
AL(OH)3 Weak bases (-OH). 1) Neutralize Slowly Usedfor symptomatic Constipation.
Taken 30 min in empty stomach. already relife of dyspepsia In renal failure,
Taken 2 hrs after meal. secreted acid. Aluminum toxicity
Antacid

Relieve heart burn immediatly. 2) Inhibit Encephalopathy


MG(OH)2 If it take with other drugs, formation of Fast Diarrhoea
It form insoluble com;ex that adsorb on pepsin
Combination Fast & Constipation + Diarrhoea = nothing
GIT wall not absorb. sustained
So, it take 2 hrs after or before other druds
Simethicone They are added to antacid either it combined or  surface tension Anti-flatulent.
Additives

no.  So, reduce buble To prevent reflux.


formation.
Alginates Form a layer of foam on the Reduce reflux
top of gastric content.
H2 Potency T1/2 Duration Inhibition of Cyto-450 is an enzyme that H2 antagonist cross placenta & are
antagonist (hrs) Cyto-450 metabolizes drugs. also secreted in breast milk.
(blokers) Cimetidine 1 1.5 – 6 1 Not used by elderly Gynecomastia.
2.3 male because it is anti- Galactorrhea.
Extremly androgenic Inhibition of Cyto-450
save drugs So, conc. of Theophyline &
Warfine.
Ranitidine 5 -10 1– 2.4 8 0.1

Famotidine 32 2.5 - 4 12 0
Omeprazole Average T1/2= 1.5 hrs. Irreversible inhibitors for
Need acidic media, So H+/K+ATPase
Lansoprazole
PPI

 Taken 1 hr befor meal.


 DoŶ’t take with other acid suppressing
agent.
Pirenzepine Inhibit gastric acid by blocking M3 Used in refractory
receptor cases that is not
muscarinic

responding to other
Anti-

drugs.
Used in nocturnal
pain.
P H R M A C O L O G Y - NOTE 3 - Treatment of Peptic Ulcer

 Muocosal protective Agents


DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
Sucralfate It is salt of ( socrose + AL(OH)3 ). 1) In acidic pH, it become
Taken 1 hr befor meal. viscous gell & protect ulcer.
Work in acidic pH 2) Stimulate PG production.
 Not used with antacid or H2 antagonist.
Misoprostol It is a PGE1 analogue 1) Gastric acid inhibition. Used with NSAID to Diarrhoea
2) Stimulate secretion of prevent peptic ulcer Abdominal pain.
mucus & bicarbonate. Abortion?
3) Enhance mucusal blood
flow.
Bismuth subsalicylate 1) Coat the ulcer Stain stools & tongue with black
2) stimulate secretion of color.
Bismuth sobcitrate mucus & bicarbonate. Cause bismuth toxicity with long
3)  PG synthesis. used.
 Drugs erdicate Helicobacter pylori
DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
Omeprazole It is combination of ONE acid suppressant + 2
Or antibiotics.
Lansoprazole (PPI) Given for 14 days.
Triple Therapy

Then, followed by PPI for 4 - 6 wks.


Clarithromycin
Amoxycillin
or
Metronidazole
Omeprazole It is combination of ONE acid suppressant + 3
Or antibiotics.
Lansoprazole (PPI) Given when triple therapy fails.
Quadruple Therapy

Bismuth Subsalicylate
Metronidazole
Tetracycline
P H R M A C O L O G Y - NOTE 4 & 5 - GIT Drugs

• It help easy evacuation of the bowel


contents during defecation.
Laxative
• Usually self-prescribed for the relief of
constipation

• It is best prevented with:


• high fiber diet.
Constipation
• adequate fluid intake.
• regular exercise.

• For mild to moderate dehydration:


• ORS (oral rehydrate salt)
• NaCl, KCl, Na HCO3
• glucose & water
Management of dehydration • For sever dehydration:
• IV fluids
• 5% dextrose & normal saline.
• KCl &/or Na HCO3, when
hypokalemia &/or acidosis
P H R M A C O L O G Y - NOTE 4 & 5 - GIT Drugs

GI Drugs

Anti-Diarrhoeal
Laxative Drugs

Simulant Balance Anti-


Bulk Formation Faecal Softners Osmotic Polyethylene glycol Opioid
Laxative Laxative muscarinics
(Bowl Cleaning
Solution)

Methyl-cellulose Liquid paraffin Bisacodyl Mg hydroxide Diphenoxylate Dicyclomine


Polyethylene
glycol

Glycerin Hyoscine-N-
Bran Loperamide
Senna Mg sulphate butyl bromiae
suppository Na sulphate

5-HT3
Ispagula husk Na sulphate Adsorbents
antagonists
Na chloride

Na citrate alosetron Kaolin Pectin Colloidal


Na bicarbonate Bismuth

Lactulose Al silicate
K chloride

Mg silicate
H2O
P H R M A C O L O G Y - NOTE 4 & 5 - GIT Drugs

 Laxatives
DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
Bulk Formation Methyl-cellulose 1) Absorb water. Constipation Intestinal obstruction
2)  the bulk of stool. Diverticular disease. Prevented by taking
Bran sufficient H2O.
3) Stimulate peristalsis. Colostomy.
Ispagulahusk Hemorrhoids & fissure.
Irritable bowl syndrome.
Faecal Liquidparaffin Given oraly. 1) Lower surface tension. Constipation (can be used in Aspiration pneumonia
Softner 2) Make stool soft. pregnant ladies) Leakage of stool.
To avoid straining at stool in Deficiency of Vit. A, D, E & K.
myocardial infarction. with long term use.
Glycein suppository It is inserted via anal canal. 1) Makes stool soft.
2) Help evacuation.
Stimulant Bisacodyl Given oraly or suppository. 1) Stimulate intestinal motility. Constipation. Diarrhoea.
laxative The onset of action 6-8 hrs. 2) Na & water absorption. Preparation for radiology. Loss of fluid & electrolyte.
The effect is repeated due to entero- Avoid in intestinal obstruction &
hepatic re-circulation. pregnancy
Senna
Osmotic Mg hydroxide Its action take 1-3 hrs. 1) Hold water due to osmotic pressure. Constipation. Diarrhoea.
2) Distend the bowl. Preparation for radiology. Loss of fluid & electrolyte.
Laxative Mg sulphate 3) Prompt evacuation. Expulsion of worms.
Na sulphate Avoid in pregnancy
Avoid Na-salts in CVS, liver & renal
Na citrate
diseas.
Lactulose Non-absorbablesugar 1) Reduces pH due to conversion of NH3 Constipation. Flatus.
to NH4. Control of encephaopathy in liver & abd cramps.
2)  absorption of ammonia. cirrhosis.  When it is l
metabolize By bacteria
in GIT.
Balanced Polyethylene glycol It is a bowl cleaning solution. It retaines H2O & electrolytes in the Bowl cleaning to prepare for:
Na sulphate It is isotonic to intestinal contents. lumen of GIT.  Surgery.
polyethyle & take faecal matter out along with it .  Colonic endoscopy.
ne glycol Na chloride  Radiology.

Na bicarbonate
Contains:
K chloride
H2O
P H R M A C O L O G Y - NOTE 4 & 5 - GIT Drugs

 Anti- Diarrheals
DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
Opioid Diphenoxylate Usually given in combination with It gonize opioid receptors (e.g. μ R). So, it. Minimal sedation.
atropine. 1) peristalsis movement. Minimal dependence.
2) constrict sphincters.
Loperamide Most their effects are on GIT.
Anti-muscarinic Dicyclomin They competitively blocking M3 NOT used with elderly patients Dry mouth.
receptors in GIT. So, theLJ… that have glaucoma Constipation.
1) peristalsis movement. NOT used with male patients that Tachycardia.
Hyoscine-N-butyl bromide 2) constrict sphincters. have prostatic hypertrophy. Palpitation.
 IOP.
Urineretention.
5-HT3 Alosetrone It is well absorbed from GIT. Competitively block 5-HT3 R. so, it… Control of sever. Constipation.
antagonists Has short T1/2. o ↓ GI ŵotility in irritable bowl syndrome which is Ischemic colitis.
Has long acting. more common in women.
Adsorbents Kaolin Al sikicate Adsorb microorganisms & toxins. Constipation.
Mg silicate Absorb water.  absorption of many
Pectin It is indigestible carbohydrate from drugs.
apple Colloidal bismuth gives
Colloidal bismuth black color to tongue &
stool.
P H R M A C O L O G Y - NOTE 4 & 5 - GIT Drugs
GI Drugs

Anti-Emetics
Drugs for IBD Prokinetic
Drugs

D2 R Anti- D2 R 5- HT4 R
Immuno- antagonists histamine antagonists agonist
5-ASA
suppresive
Metoclopr- Metoclopram Metoclopram
Cyclizine
amide ide id
Gluco- Cytotoxic Cytokine Azo-
Mesalamine
corticoids agents Inhibitors compounds
Domperi-
Meclozine Domperidone
done

Prednisone Azathioprine Infliximab Sulfasalazine


Diphenhydr-
Droperidol
amine

Prednisolon Methotraxate Olsalazine Anti-


Phenothiazines
muscarinics

Promethazine Hyoscine
budesonide Balsalazide

5-HT3 Marijuana
antagonists derivatives
Hydrocortisone

Ondansetron Dronabinol

Nabilone

Steroids

Dexamethne
P H R M A C O L O G Y - NOTE 4 & 5 - GIT Drugs

 Treatment of Inflammatory Bowel Disease


DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
Sulfasalazine 5-ASA + sulfapyridine. 1) 5-ASA iŶhiďits…… 1st line drugs for treatment of GIT: Nausea, vomiting.
 Cyclo-oxygenase enzymes. mild to moderate Hematological:
 Lipo-oxygenaseenzymes.  Ulcerative colitis.  BM suppression.
2) anti-inflammatory action.  ChroŶ’s disease  Megaloblastic anemia.
in colon or rectum. Renal:Crystal urea & Renal
Azo-compound

Azo-bond broken in stones.


GIT(colon) by azo- Hypersensitivity:
reductase that secreted  Skin rash.
by bacteria  Angiodema.
General: Headache, malaise,
5-ASA

arthralgia & myalgia.


Olsalazine 2 molecules of 5-ASA. Diarrhoea.

Balsalazide 5-ASA & amino-benzoyl


alanine.
Mesalamine Enteric coated form of 1st line drugs for treatment of Renal damage.
Mesalamine

5-ASA. mild to moderate


It available as enema &  Ulcerative colitis.
suppository.  ChroŶ’s disease
in colon, rectum or small
intestine.
Gluco- Prednisone They given oraly. • Anti-inflammatory & immune suppressant action. For acute & sever ulcerative Hypertension
corticoid So, it….. colitis & ChroŶ’s disease. Hyperglycemia.
Prednisolone peptic ulcer.
1) phospholipae A & C.
Budesonid 2) synthesis of PGs & leukotrienes synth Infection.s
of cytokines (TNF- , IL-1), chemokine Renal suppression.
Hydrocortisone Given IV injection. (IL-8.)  Prevented by terminate
3) Destroy lymphoid cells & some T-cells the treatment with
Immuno-suppresive drugs

tapering doses.
Cytotoxic Azathioprine Purine analog. 1) DNA synthesis. Alternate or additional therapy for Nausea.
2) Damage lymphoid & T- cells.  Refractory ulcerative Vomiting.
colitis. BM depression.
Methotraxate 1) Inhibitor of dihydrofolate reductase.  ChroŶ’s disease. Infections.
2) DNA synthesis. Infertility.
3) Damage lymphoid & T- cells.

Cytokine Infliximab Enteric coated form of 1) Anti- TNF(pro-inflammatory cytokine) Alternate or additional therapy for Infections
inhibitor 5-ASA. 2) release of cytokines from inflammatory cells  Refractory ulcerative Infusion reaction.
It available as enema & colitis. Feve.
suppository.  ChroŶ’s disease. Chills.
Urticaria.
Chest pain.
Dyspnoea.
P H R M A C O L O G Y - NOTE 4 & 5 - GIT Drugs

 Anti-emitic
DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
D2 receptor Metoclopramide 1) Inhibit D2 receptors in CTZ. Extrapyramidal reaction.
antagonists 2) Control vomiting . Diarrrhoea.
3) Have prokinetic effect.
Domperidone DoŶ’t crossBBB.

Droperidol 1) Inhibit D2 receptors in CTZ. Sedation.


2) Control vomiting . Extrapyramidal reaction.
 QT-interval & cause
ventriculartachycardia.
Anti-histamines Cyclizine Inhibit H1 & M3 receptors iŶ… Sedation.
Meclozine CTZ. Anti-muscarinic side effects:
Vomiting center.  dryness of mouth.
Diphenhydramine  Tachycardia.
Phenothiazines Promethazine Inhibit D2,H1 & M3 receptors iŶ…  Constipation.
CTZ.
Vomiting center.
5-HT3 receptor Ondansetron Inhibit 5-HT3 receptors iŶ… in sever vomiting e.g. in cancer
antagonists CTZ. chemotherapy.
Vomiting center.
Marijuana Dronabinol Inhibit vomiting center by stimulation of Euphoria.
derivatives cannabinoid ( CB1 ) receptors.
Nabilone Mood disturbances.
Steroids Dexamethasone • to supplement the effect of other
drugs in sever vomiting.
 Prokinetic
DRUGS PHARMACOKINETIC ACTION USES SIDE EFFECT
D2 receptors Metoclopramide 1) Blocking D2 receptors in GIT. . Extrapyramidal reaction
antagonists &   cholinergic activity in upper GI (pro-  Tremors.
5-HT4 receptors kinetic).  Dyskinesia.
agonists 2) Blocking D2 receptors in CTZ. Gynecomastia.
 control vomiting (anti-emetic) Irregularmenstrual.
3) Activates 5-HT4 receptors. ↑ prolaĐtiŶ seĐretioŶ.
Diarrhoea
Domperidone DoŶ’t crossBBB. 1) Blocking D2 receptors in GIT. Diarrhoea
  cholinergic activity in upper GI (pro-
kinetic).
2) Blocking D2 receptors in CTZ.
 Control vomiting (anti-emetic).
P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs

SEDATIVE & HYPNOTIC DRUGS

5-HT R β-adrenergic R
BNZ Barbiturates
Agonists Other Z-Hypnotics
blockers

Intermediat Intermediat Anti- Chloral


Long acting Clonidine
Short acting Long acting Buspirone Propranolol histamines Zaleplon
acting acting Hydrate

Chlordiazepox Diphenhydra
Alphazolam Oxazepam Phenobarbital Secobarbital Zolpidem
ide mine

Ultra-short
Diazepam Lorazepam Triazolam Short acting
acting
• drugs that produce
Sedatives calm & relaxation.
Clonazepam Hexobarbital Thiopental
• used for anxiety.

• drugs that put user


Hypnotics in sleep.
• used for insomnia.
DEATH
coma both of them
anesthesia
depress CNS but
Hypnotic more
hypnosis

sedation
P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs

 Benzodiazepines (BNZ)
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Chlordiazepoxide Absorption Mechanism of action 1) Sedativepreoperatively. Drowsiness.
Orally / I.M. / I.V. BNZ hyperpolarizes the membrane of 2) Epilepsy in emergency. Confusion.
(1-3 days)
Long acting

Diazepam the post-synaptic neurons by: 3) Treatment of muscle plasticity in cerebral Amnesia.
Distribution Binding to GBC binding site. palsy & tetanus Impairment of motor
Pass BBB & placenta.  affinity of the R to GABA. coordination.
Clonazepam
Secreted into breast milk.  Cl+ permeability. Dependence & addiction.
Hyperpolarize the
Alphazolam Metabolism membrane. 1) Sleep disorder, insomnia.
Inhibition of the neurons. 2) Control alcohol withdrawal symptoms.
It is done by hebatic microsomal system.
3) Treatment of muscle plasticity in cerebral
Themetabolites: Psychological dependence.
Action palsy & tetanus
o Active. Stop administration cause:
Intermediate acting

o Have longer T1/2. 1) Reduction of anxiety. Craving.


2) Sedation which encourage sleep by:
(10-20 hrs)

o Cause hangover effect.


Lorazepam The T1/2 depend on the metabolism not  latency. 1) Short term relief of sever anxiety. Physical dependence.
excretion.  non-REM. 2) Sleep disorder, insomnia. Stop administration cause
 REM. 3) Control alcohol withdrawal symptoms. withdrawalsymptoms:
Excretion 3) Reduction of muscle tone & 4) Treatment of muscle plasticity in cerebral Insomnia.
It is done by kidney. coordination. palsy & tetanus Anxiety.
 4) Anti-convulsant.
Autonomic over activity.
5) Prolonged sleep with over dose.
It safe on over dose if it taken alone.  HR & BP.
It is the most widely used sedative because: 6) Tolerance. Tremors.
Oxazepam High Ti. It is pharmacodynamic ( 1) Sleep disorder, insomnia. Diaphoresis.
Low risk of dependence. the sensitivity of the 2) Control alcohol withdrawal symptoms. Muscle cramps.
Short acting

receptors).
(3-8 hrs)

Acute overdose or toxicity is treated 3) Treatment of muscle plasticity in cerebral Confusion.


by: Develop after chronic use palsy & tetanus. Seizures.
FLUMAZENILE. (1-2 wks).
Triazolam Irritability.
Ataxia.

Anxiety
 Fear-induced situation. Uses of BNZ
 It has: 1) Short term relief of sever anxiety.
 CNS symptoms: 2) Sedativepreoperatively.
Insomnia. 3) Sleep disorder, insomnia.
Anorexia. 4) Epilepsy in emergency.
Muscle tension. 5) Control alcohol withdrawal symptoms.
 Peripheral symptoms: 6) Treatment of muscle plasticity in cerebral
Sweating. palsy & tetanus.
Tremors.
Palpitation.
P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs

 Barbiturates ( acids)
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Thiopental Absorption  Depression of the neural activity by : NOT used as sedative or hypnotic drugs but Death in high dose due to:
Ultra-Short

Orally / I.M. / I.V.  Enhancement of they are only used for: CVS depression.
acting

GABAergicpathway. 1) I.V. anesthesia. Respiratory depression


Distribution  Blocking excitatory NT. 2) Epilepsy. Dependence.
To all body 3) Hyperbilirubinemia. Drug-druginteraction.
Hexobarbital Metabolism Paradoxical excitement of
acting
Short

It is done by hebatic microsomal system. children.


This system cause drug-drug iteractoin. Prolonged hangover.
NOT used as sedative or hypnotic drugs but Porphyria.
Secobarbital Excretion they are only used for: Tolerance
Intermedia
te acting

It is done by kidney. 1) Epilepsy. It is pharmaco-


It is pH dependence. 2) Hyperbilirubinemia. dynamic(enzyme
Alkalization of urine with NaHCO3 enhance induction).
barbiturates renal execrerion.
Phenobarbital  So, used for treatment of
Lon

acti
g

overdose.
 5-HT Receptors Agonists
Buspirone Mixed agonist- antagonist.  Anxiolytic action ( 1-3 wks).  Generalizedanxiety. Nervousness.
Minimal risk of dependence.  Little sedation. Dizziness.
 Little impairment of coordination. Headache.
 Minimal risk of dependence. Nausea & vomiting.
 NO hypnotic , NO euphoria.
 β-adrenergic Blockers
Propranolol non-selective β-blocker. 
peripheral symptoms of anxiety 1) Anxiety. 
 Sweating, Tremors & 2) Social phobia.
Palpitation. 3) NOT for (asthma, COPD, diabetes)
Reduce performance anxiety such:
 Public speech or Interview.
 Other sedative & hypnotic
Diphenhydramine  Anti-histamine. Has anit-cholinergic action. 1) Insomnia. 
Anit-H

2) Anxiety & agitation.

Chloral Hydrate  Used to induce sleep in children 


to perform certain medical
procedure.
Clonidine  α2 agonist.  1) Control sympathetic overactivity 
associated with:
Narcotic withdrawal.
Acute anxiety.
2) Panic attack of anxiety.
P H R M A C O L O G Y - NOTE 6 - Sedative & Hypnotic Drugs
 Z-hypnotic
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Zaleplon  Selective for α1 subunite of BNZ receptor  Depression of the neural activity by
comlex. enhancement of GABAergic pathway.
1) Less risk of tolerance.
2) Less risk of amnesia.
3) Minimal rebound:
Zolpidem Insomnia.
Anxiety.
Hagover effect.

 The acton is antagonized by


Flumazenil
 that impact sleep stage.
P H R M A C O L O G Y - NOTE 7 - General Anesthesia

GENERAL ANESHESIA
DRUGS

I.V. GA Inhalational GA

Thiopental GAS Volatile Liquids

Midazolam Nitrous Oxide Halothane Enflurane Isoflurane Sevoflurane

Fentanyl

anesthesia •loss of
sensation
Ketamine

•drugs that
anesthetic drug produce loss
of sensation
Etomidate
•produĐe loss of

GA all sensation
with loss of
consciousness
P H R M A C O L O G Y - NOTE 7 - General Anesthesia

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT


Thiopental It is a barbiturate drug.  Induction of GA.  Respiratory depression.
Fast onset.  NOT used in asthmatic patients.  Bronchospasm.
because lipid solubility & cross BBB.  CVS
Ultra-short acting. BP.
due to fast redistributed to tissues out Cardiac Output
side the brain.  porphyries
Slowlymetabolized.
Narrow margin of the safety.
Etomidate moremetabolized.  Induction of GA.  Involuntarymovement.
Cause low risk of CV &R depression.   adrenocortical response
to stress.
Intravenous

 Post-operative nausea &


vomiting.
Midazolam It is a BNZ drugs.  The action make little changes in Basal anesthesia.  Amnesia.
Ultra-short acting. BP. Anxiety.
To accelerate the recovery from anesthisea, Ventilation. Anesthesia for patient with:
Use Flumazenil. myocardial diseases.
hypovalemicshock.
Ketamine Mainly in pediatrics for minor surgery.  Post-operative
Basal & dissociative anesthesia. hallucination in adult.
Anesthesia for hypovalemic shock patient.  Amnesia.
 BP &HR
Fentanyl  Analgesic by using (Fentanyl + Bronchoscopy.
Droperidol). Cystoscopy.
Nitrous Oxide Administration  Low potency (MAC=100).  With prolonged use
Mixed with water.  It is combined with other inhalation A. Leucopenia.
Gas

Taken by inhalation.  Rapid induction & recovery. Megalobalstic anemia.


Distribution  It has analgesic property.
It is well distributed & determines  It has low lipid solubility in brain.
Halothane  Speed of duration.  Most widely used. All the volatile liquid anesthesia:  Hypotension.
 Speed of recovery.  High potency (MAC=0.7).   myocardium contractility.  Uterine relaxation &
Metabolism  It has weak analgesic property.  Bradycardia. bleeding.
Inhalational

It is the major responsible for side effect. o It leads to cardiac  Cardiacdysrhythmia.


Ex: Methoxyflurane 
dysrhythmia.  Liver toxicity.
Volatile liquids

o Treated by Atropine.
Enflurane Fluoride + Oxalate (nephrotoxic).
Ex: Halothane 
Isoflurane Bromide + Triflouroacetate  Faster induction & recovery. Heart suergery.
(hepatotoxic).  Has muscle realaxing property.
sevoflurane  Rapid induction & recovery. Induction of A in children.
Elimination
Suitable for heart surgery.
Clearance is mainly by lung.
 Because it has minimal effect on CVS.
It determines the duration & recovery.
Methoxyflurane  Nephrotoxicity.
P H R M A C O L O G Y - NOTE 7 - General Anesthesia

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT


I.V. They have narrow Ti. Mechanism of action Respiratory depression.
So, the dose must be calculated accurately. They depress the activity of the Bradycardia.
neurons in the brain. Liver toxicity.
By activate inhibitory Kidney toxicity.
pathway (GABA & Glycine). Cough.
Site of action: Salivation.
Reticular formation. Vomiting.
Hippocampus.
Inhalation They have narrow Ti. Cortex.
So, the dose must be calculated accurately. Action
The dose is measured by MAC value. Depression of all CNS function.
MAC: On CVS:.
o It is the concentration of anesthetic that o  myocardium contractility.
GA

result in immobility in 50% of patients On RS: all GA (excepte N2O)


exposed to a painful stimulus. o  respiration.
o It measure: o  arterial Pco2.
Dose. o  ventilation in response to
Potency. hypoxia.
o  mucociliary function.
o Post-operative R infection
with long use.
Nephrotoxicity.
On Liver:
o  blood flow
o Hepatotoxicity.
On uterus:
o Relaxation  bleeding.
INFLUNCING FACTORS FOR THE SELECTION OF GA COURSE OF ANESTHESIA
Patient's factors 1 Anesthetic premedication.
1 Age Diazepam Produce sedation
Relief anxiety Reduce GA dose
2 Allergy history Morphine Produce analgesia
3 Status of organ system (e.g. RSD, CVSD, NSD, Endocrine D, Liver &kidney D) Atropine Reduce side effect of GA
4 Genetical diseases (e.g. porphyria) Metoclo- Produce anti-emetic effect
5 Use of other drugs proamide Prevent aspiration
Anesthetic factors (criteria of ideal anesthetic) Because no GA has all 2 Induction of GA
1 Rapidly & smooth induction these criteria, I.V. GA loss of all sensation & loss consciousness
We use 3 Maintenance of GA & muscle relaxant
2 Fast recovery
combination A
3 Has muscle relaxing property Inhal. GA maintain anesthesia
4 Wide margin of safety Tubocuraine muscle relaxant
5 Minimum side effects 4 Recovery ( by terminate inhaler A)
P H R M A C O L O G Y - NOTE 8 - Local Anesthesia

LOCAL ANESHESIA

weak Potency & short Duration moderate Potency & intermediate high Potency & long Duration
Duration

Lidocaine (Xylocaine) Tetracaine

Procaine Chloroprocaine
Mepivacaine
Bupivacaine

•produĐe local loss

LA of sensation
without loss of
consciousness
Prilocaine Etidocaine

•ProĐaiŶe
•ChloroproĐaiŶe
•Tetracaine
•BeŶzoĐaiŶe Ropivacaine
•BeŶodžiŶate
•LidoĐaiŶe
(Xylocaine)

Amide •MepivaĐaiŶe
•BupivaĐaiŶe
•EtidoĐaiŶe
P H R M A C O L O G Y - NOTE 8 - Local Anesthesia

DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT


Procaine Administration Mechanism of action 1) Surface anesthesia: Usuallyminimum,
Weak Potency &


short duration

Local injection. LA block nerve conduction (initiation o on Skin (wound & ulcer) because:
Local application ( solution, powder & propagation of AP) by: o on MM (mouth or nose). o Applied locally.
or cream) Binding to Na+ channels & o in Ophthalmology (corneal A). o Combinewd with
Chloroprocaine
prevent Na+ permeability. o powder, solution creams or ointment vasoconstrictors.
Absorption are used.
NOT desirable because: Action 2) Infiltration anesthesia.
Lidocaine  It  duration.  LA are lipid soluble / weak base. o as in (wound suturing, cyst removal). 1)Hypotension.
Moderate Potency

(Xylocaine)  It   3) Individual nerve block anesthesia. 2)Bradicardia.


& Intermediate

systemic side effects. At pH= 7.4,


o as in Dental anesthesia. 3)CNS:
duration

o they are UNIONIZED molecule.


Mepivacaine Metabolism o They pass lipid membrane. 4) Spinal Epidural anesthesia. Tinnitus.
Easter, fastly metabolized by tissues &  When reach the cytoplasm, o as in surgery of (LL, abd, pelvis, Lightheadness.
plasma esterase. o They become (ionized + rectum). Headache.
Prilocaine  Into PABA (cause allergy). unionized). 5) Treatment of cardiac dysrhythmia. Convulsion.
 Short duration. o The IONIZED molecules: 4)Allergy (in ester type).
Tetracaine 1) Infiltration anesthesia.
Amides, slowly metabolized by liver Bind to Na+ channels.
o as in (wound suturing, cyst removal).
High Potency &

microsomal enzymes. Block Na+ influx.


long duration

Bupivacaine 2) Individual nerve block anesthesia.


 Longer duration. Prevent AP.
o as in Dental anesthesia. Side effects occur due to:
. 3) Spinal Epidural anesthesia.
Etidocaine  The action are susceptible for (small o High dose.
o as in surgery of (LL, abd, pelvis,
diameter / unmylinated) fibers more o Injected into BV.
Ropivacaine rectum).
than (large diameter / mylinated) They are potent & have
4) Treatment of cardiac dysrhythmia.
fibers. long duration.
Benoxinate  It is ester LA. In ophthalmology for corneal A because :
 NO mydriasis.
 NO corneal injury.
Benzocaine Used as powder or cream. Surface anesthesia on Skin (wound & ulcer) 
Because it is insoluble, it produces less
systemic toxicity.
INFLUENCINGFACTORS
IF Advantage Disadvantage
1 Dosage High Fast onset / long duration 
side effect
2 Site BV 
side effect / Short duration
3 Lipid solubility LS 
effect
4 Infection/ pH action / ionized /effect
inflammation Vaso- 
absorb /  side effect/
dilation
duration
5 Type of solution Alkali Less painful / fast onset /
non-ionized /  action / effect
6 +vasoconstrictors duration/ absorb /side effect
P H R M A C O L O G Y - NOTE 9 - Opioid Analgesics (Nacrotic analgesic)

OPIOID ANALGESICS DRUGS

pure Agonist patial Agonist Atagonist

Morphine Nalorphine Pentazocainel Naloxone

Methagone

Codeine

Pholocodeine

• Mu
Dextropropoxyphene
Classes of Opioid Rs •Kappa
•Delta
Diphenoxylate

place of Opioid R •CNS


Loperamide •Periphral tiissues

Noscapine •agonist if it is combined


partial Agonist with pure agonist.
(mixed agonist-antagonist) •antagonist if it is combined
Fentanyl with antagonist.
P H R M A C O L O G Y - NOTE 9 - Opioid Analgesics (Nacrotic analgesic)

DRUG PHARMACOKINETIC USES ACTION SIDE EFFECT


Morphine Administration Strong analgesic for chronic pain (cancer). On CNS. Dysphoria.
All taken by orally. MI ACTION MECHNISM Respiratory depression.
Sustained release formulation. Add with inhaler GA to produce analgesia. 1 Analgesia Nausea & vomiting.
Morphine is given by I.V. Manegment for dyspnea. 2 Euphoria  prominent with pain  intra-cranial pressure.
Methadone o 75% of it, become inactive Strong analgesic for chronic pain (cancer). 3 Dysphoria Constipation.
Meperidine after absorption Strong analgesic for chronic pain (cancer). Urinaryretention.
Distribution Analgesic for labor pain. Allergy:
Add with inhaler GA to produce analgesia. Itching.
They are well distributed.  Bronchospasm.
st It is lipid soluble. Moderate analgesic for chronic pain (cancer) Trancealrigidity(back
n Codeine 4 Resp. 
sensitivity of RC to CO2
s
i 5 Nausea stimulation of CTZ Vomiting
go
e hydrocodeine 6 Miosis agonize R on III c.n.
A
r Antitussive
u
P They cross BBB & placenta. Cough suppression. 7 depress the CC pain)
Moderate analgesic for chronic pain (cancer 8 
BP & VD Depress VMC
Metabolim On CVS. ( in large iv
Pholocodeine Cough suppression
dose) By microsomal system
Dextropropoxyphen BP depress VMC 
VD
The metabolites are active.
Noscapine Heroin (diacetylmorphine)
Morphine. direct VD effect
Diphenoxylate Codeine (Methylomorphine) Morphine. Treatment of diarrhea. release of histamine VD
Loperamide The metabolite are conjugated. On GIT.
Fentanyl Add with inhaler GA to produce analgesia. 1 Constipa- sphincter tone
Elimination tion s.m. motility
Mainly by kidney. 2 intra- spasm of bile duct
USES COTRA-INDICATION billary P spasm sphincter of oddi Treatment of addication
1) Analgesic for acute & chronic sever pain. 1) Head injury. On UT. Clonidine.
a. Acute pain (MI , post-operative) Miosis. 1 spasm of ureters Control withdrawal
b. Chronic pain (cancer)  Resp. 2 Constriction of U sphincter symptom.
c. Labor pain 2) Biliary & renal colic(ex Meperidine) 3 micturation reflex
2) Cough suppression. 3) Respiratory diseases. Tolerance & Dependence. Methadone
3) Treatment of diarrhea. effect with repeated administration
4) Mangment of dyspnea. (asthma & COPD)
1 Analgesic Rapid tolerance
5) Analgesic with GA 4) Acute abdomen pain.
Interfere with proper 2 Resp. Slow tolerance
a. Add with inhaler GA 3 Miosis NOT develop
diagnosis.
Acute MORPHINE poisoning 5) Pregnancy & labor (ex Meperidine) 4 constipation
5 convulsion
Manifestation: Treatment Addict fetus.
Coma / pin point pupil 1) Artificial respiration. Neonatal asphyxia. 6 Cross tolerance occur different agonist
Hypoventilation & hypoxia 2) Stomach wash. 6) Liver diseases Addcation.
Hypotension 3) Repeated I.V. Deficient metabolism Physical D Sudden withdrawal lead to
Hypothermia Naloxone Psycho. D withdrawalsyndrome
P H R M A C O L O G Y - NOTE 9 - Opioid Analgesics (Nacrotic analgesic)

DRUG PHARMACOKINETIC USES ACTION SIDE EFFECT


Pentazocine Agonist on Kappa R. Analgesia. Dysphoria.
Partial agonist on Mu R. Psychomimetic effect.
Cause weak  RC. Anxiety.
Milddependency. Nightmares.
Hallucination.
Partial Agonists

Mildwithdrawal manifestations.
Withdrawal manifest.
with morphine addict.
Buprenorphine Maintainance drug for opioid dependent Psychomimetic effect.
patient. Anxiety.
Nightmares.
Nalorphine Hallucination.
Withdrawal manifest.
with morphine addict
Naloxone Acute opiod poisoing Reverse sever respiratory depression.
Antagonist
Pure
P H R M A C O L O G Y - NOTE 10 - Anti-Psychotic Drugs
ANTI-PSYCHOTIC DRUGS

Typical Atypical

Phenothiazines Thioxanthines others Risperidone

Flupenthixol Haloperidol Quetiapine


Group 1 Group 2 Group 3

Chlorpromazine Pericyazine Fluphenazine Zuclopenthixol Pimozide Olanzapine

Trifluperazine Sulpiride Clozapine


•SĐhizophreŶia
•BraiŶ damage
Psychoses are: •MaŶia
Aripiprazole
•TodžiĐ delirium
•Agitated depression

•ŵaŶifest disorders of
•perĐeptioŶ
Schizophrenic •thiŶkiŶg •+ve •delusioŶs •SoĐial/oĐĐupatioŶal
dysfunction

Negative symptoms of
•speeĐh symptoms •halluĐiŶatioŶs
patients

Positive symptoms of
•eŵotioŶ Schizophrenia has •-ve •disorgaŶized •laĐk of self care
•phLJsiĐalactivity speech
symptoms

Schizophrenia
Schizophrenia
•NeuroleptiĐs •ĐatatoŶia
•due tp neurological effects e.g. •agitatioŶ
Antipsychotic Parkinsonism
•MiŶor tranquilizersas
drugs are called •du to Đalŵ oƌ ຃tƌaŶƋuilizeຄ
psychotic symptoms without loss
of consciousness
P H R M A C O L O G Y - NOTE 10 - Anti-Psychotic Drugs

 Typical Anti-Psychotics
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
G1 Chlorpromazine Taken Orally. Mainly antagonize D2 receptors. • Dopamine hypothesis for ANS
schizophrenia:
Phenothiazines

Some of them may also antagonize 5-HT2 Anti-muscarinic


G2 Pericyazine receptors • Increased dopamine blurred vision, IOP.
More effective in the control of positive receptor density in dry mouth,HR, confusion.
symptoms mesolimbic-frontolarea constipation, urine retention
G3 Fluphenazine Given I.M. Inj. /3-4 wks in schizophrenics
Cause more extrapyramidal side effects α – blocking
• Most antipsychotic drugs ejaculation & impotence.
Trifluperazine Taken Orally. block Dopamine D2 HR & orthostatic BP.
receptors in brain CNS
Flupenthixol Given I.M. Inj. /3-4 wks • Successful treatment of D R blocker
schizophrenia reduces Parkinsonism.
Thioxanthines

homo-vanilic acid (HVA), Akathesia.


a metabolite of Dystonia
dopamine in CSF Super sensitivity of D R
Zuclopenthixol Taken Orally.
• Drugs that increase Tradive dyskinesia.
dopamine activity like Sedation.
levodopa, cocaine, Toxic confusional state.
apomorphine & Neuroleptic malignant
Haloperidol Given I.M. Inj. /3-4 wks amphetasmines syndrome.
aggravate schizophrenia Endocrine(due to DR block &
or produce psychosis prolactin)
• There is possible Female
Pimozide Taken Orally.
involvement of other Amnorrhra & galactorrhea.
neurotransmitters also Male
others

likeglutamate, Gynecomastia & impotence.


Sulpiride serotonin, histamine, etc
e.g. Glutamate receptor Weight gain (appetite).
(NMDA-receptor) antagonist Hyperglycemia.
(phencyclidine) can produce Cholestatic jaundice.
schizophrenia like state Cataract.
& atypical anti-
Risk of teratogenecity.
psychotics also inhibit 5-HT2 & D4
receptors

DRUGS sedation anti-muscarinic extra-pyramidal PATHO-PHYSIOLOGY OF SCHIZOPHRENIA


side effects side effects
G1 Marked Moderate Moderate dopamine receptor density in mesolimbic-frontol area in schizophrenics.
G2 Moderate Marked Less dopamine activity by drugs (like levodopa, cocaine, apomorphine & amphetasmines) that
G3 Less Less Marked aggravate schizophrenia or produce psychosis.
Thioxa. NT (like glutamate, serotonin, histamine) that agonist 5-HT & D receptors.
others Successful treatment of schizophrenia reduces homo-vanilic acid (HVA) in CSF.
P H R M A C O L O G Y - NOTE 10 - Anti-Psychotic Drugs
 Atypical Anti-Psychotics
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
st
Risperidone Block both D2 & 5-HT2 receptors. Schizophrenia (1 line Anti-muscarinic & prolactin related se

 less extra-pyramidal &


Given I.M. Inj. /3-4 wks

prolactin related side


Relive both + &- symptoms. drug) Less extra-pyramidal se.
Weight gain.
Relatively low affinity for May cause:
dopaminereceptors  Anxiety.
 Insomnia.

effects
Also or receptors
 Dizziness.
 BP
Quetiapine They metabolized by P-450 in the liver. Anti-muscarinic & prolactin related se

 More effective in the control


Drug interactions occur with enzyme inducers Less extra-pyramidal se.
& inhibitors. Weight gain.
Olanzapine

of negative symptoms
May cause:
Drowsiness.
Headache.
Hyperglycemia (by olanzapine)
Clozapine Resistant Schizophrenia Agranulocytosis (1st 3 m).
(2nd line drug) So, monitor WBC count:
before start.
every 2 wk for 6 m
Aripiprazole partial agonist at D2 receptors. α – blocking
Antagonist at 5-HT2 receptors. orthostatic BP.

& 5-HT2 receptors


antagonize D2, D4
D2 R blocker
Tradive dyskinesia.
Neuroleptic malignant
syndrome
Weight gain.
Hyperglycemia.
PHARMACOKINETIC ACTION OF DOPAMINE RECEPTORS MECHANISIM OF ACTION of anti-psychotic drugs
Administration Metabolism
Taken Orally. It occur in liver & subject to 1st R Action Adenyl- cAMP SITE OF D2 RECEPTORS EFFECT
The bioavailability is good pass effect. via cyclase
Some are taken I.M inj. D1 Gs Activated  Mesolimbic-Mesocortical anti-psychotic
Drug interactions pathway
Distribution  activity of anti-Parkinsonism drugs D5
High lipid solubility. that are DA agonists (levodopa, D2 Gi Inhibited  Nigro-Striatalpathway Extra-pyramidal
Taken 1-2/d due to long T1/2. amantadine, bromocriptine), D3
due to blocking of D2R D4 Tubero-Infundibular ↑ prolactin secretion
Potentiate sedative effects of pathway Galactorrhea
benzodiazepines & Medullary-Periventricular appetite
antihistamines pathway
May interact with liver CTZ Anti-emetic
P H R M A C O L O G Y - NOTE 11 - Anti-Depressants Drugs

ANTI-DEPRESSANT
DRUGS

ARI MAOI

Selective
Tricyclic Heterocyclic SNARI SSRI Tranylcypromine
NERI

Amitriptyline Amoxapine Venlafaxine Fluoxetine Imipramine Selegiline

Nortriptyline Maprotiline Fluvoxamine Atomoxetine Moclobemide

Imipramine Trazodone Citalopram


• 
action of Tyramine
MAOI cause (sympathomimetics)
• Serotonin syndrom with SSRI

Clomipramine Bupropion Sertraline • does not cause


selective MAO-B I tyramine related
reactions
• hyperthermia.
Serotonin • muscle rigidity.
• myoclonus.
• griefe •biochemical • bipolar syndrom has
Endogenous (melanocholic)

• CVS & Resp. failure.


disorder affective
Reactive (secondary)

• illness
Manic-depression

(genatically) disorder •due to depletion


•iŶaďilitLJ to depression of amine stores in
cope with CNS
no
depression

is s
e minor life
pr events
de
P H R M A C O L O G Y - NOTE 11 - Anti-Depressants Drugs

 Amine Re-uptake Inhibitors (ARI)


DRUG PHARMACOKINETIC MECHANISM OF ACTION USES SIDE EFFECT
Amitriptyline Caution in glaucoma & BPH  re-uptake of NE & 5-HT. Depression. Anti-muscarinic
due to anti-muscarinic side effect. also concentration in synapse. Anxiety disorders. blurred vision, dry mouth.
anti-depreesant

Nortriptyline Caution in driving & skill full word Chronic pain. HR, confusion.
due to sedation Enuresis. constipation, urine retention.
Tricyclic

Imipramine α – blocking
ejaculation & orthostatic BP
sedation.
Clomipramine
Seizure.
Weight gain.
Sex disturbances.
Amoxapine 
re-uptake of NE & 5-HT. Depression. Parkinsonism. moderate
anti-depreesant


D2 receptors. Anxiety disorders Akathesia. sedation
Heterocyclic

So, it acts as anti-psychotic prolactin. &


Maprotiline 
re-uptake of NE & 5-HT Seizures. anti-
Arrhythmias muscarinic
Trazodone Induce sleep.
Bupropion 
re-uptake of NE, 5-HT & DA. Seizures.
 Aggravate psychosis.
Venlafaxine Low dose acts as SSRI. 
re-uptake of 5-HT (& NE but less). Depression. Low dose
5-HT & N-ad RI

High dose 
acts as TSAs Anxiety disorders. o Sedative & anti-muscarinic.
(SNARI)

Chronic pain High dose


o Sedative & anti-muscarinic.
o Nausea.
o  BP
o Sex distrabunces.
Fluoxetine 
re-uptake of 5-HT (more selective). obsessive & compulsive D Transient nausea.

depression
Bulimia Libido. (initial)

anxiety
SSRI

Fluvoxamine obsessive & compulsive D Sex dysfunction. (maintenance


Citalopram therapy)
Sertraline
S NERI Imipramine 
re-uptake of NE (more selective). Attention deficit hyperkinetic
Atomoxetine disorder.
 Mono-Amine Oxide Inhibitors (MAOI)
DRUG PHARMACODYNAMIC MECHNISM OF ACTION USES SIDE EFFECT
Tranylcypromine Inhibits MAO-A & MAO- B. They metabolism of amines by MAO.  Headache.
 duration of action of Drowsiness.
Selegiline Inhibit MAO- B. NE, 5-HT & DA. Weight gain.
also concentration. Postural PB.
o MAO-A metabolizes NE , 5-HT & Tyramine. Sex disturbances.
o MAO-B metabolizes DA more than others.
P H R M A C O L O G Y - NOTE 14 - Treatment of Epilepsy
ANTI-EPILEPTIC DRUGS

Partial seizures & Generalized seizures Others


gneralized tonic-clonic

Old Drugs Newer Drugs Ethosuximide Phensuximide Acetazolamide Benzodiazepines

Phenytoin Lamotrigine Trimethadone Oxazolidinediones Diazepam

Carbamazepine Gabapentine Lorazepam


• motor area (convulsion)
• hypothalamus (autonomic discharge)
Involvement of • reticular formation (unconsciousness)
Valporate Topiramate • Repeated seizure activity leads to Clonazepam
neurodegeneration due to excitotoxicity

Barbiturates Vigabatrine
Focal Seizures •reŵaiŶslocalized
Nitrazepam

Generalized •priŵarLJ (involve all cortical neurons) Clorazepate


Levetriacetam •seĐoŶdarLJ (spread afterward)
Seizures Dipotassium

• inhibitory NT.


• excitatory Nt
Felbamate TREATMENT •alter the permability of membrane
Clobazam
to ions (Na, K or Ca)

Zonisamide
Tiagabine

SEIZURES
•siŵple;ĐoŶsĐiousŶessͿ •GeŶeralized tonic-clonic (grand mal)
GENERALISED
PARTIAL SEIZURES

•Đoŵpledž(unconsciousness) •AďseŶĐe (petit mal)


•PS secondarily generalized •ToŶiĐ , Atonic , Clonic & Myoclonic
seizures
•IŶfaŶtile spasm
P H R M A C O L O G Y - NOTE 14 - Treatment of Epilepsy
 Partial seizures & generalized tonic-clonic
DRUG PHARMACOKINETIC MECHANISM OF ACTION USES SIDE EFFECT
Phenytoin It is metabolized in the liver.  Block or alter Na-voltage channels. 1) Partial seizures DOSE DEPENDENT
plasma conc. <10 mg/L .  At high concentration: 2) Generalized tonic-clonic seizures. Acute effect
1st order kinetics. Inhibit release of NE & 5-TH. 3) Status epilepticus. Nystagmus.
plasma conc. = 10-20 mg/L . Inhibit MAO activity. 4) Trigeminal neuralgia (2nd choice). Diplopia.
zero order kinetics. Promote uptake of 5) Cardiacarrhythmia. Ataxia.
The metabolism is inhibited by: Dopamine Lethargy.
Sedation.
o Na valporate.
Chronic effect:
o Cimetidine.
Gingival hyperplasia, Hirsutism , Acne
o Isoniazide.
Nausea ,vomiting ,epigastric pain, anorexia.
o Chloramphenicol.
Megaloblastic anemia.
o Co-trimoxazole.
Mild peripheral neuropathy
It is a inducer of HME. Osteomalacia.
So, it enhances metabolism of: Hemorrhagic diseases of new born.
Carbamazepine Fetal Hydantoin syndrome.
Warfarin,Steroids. HYPERSENSITIVITY
TCA & OC Agranulocytosis with fever, rash , SLE & fetal hepatic
necrosis.
Carbamazepine  Block Na-voltage channels. 1) Partial seizures DOSE DEPENDENT
 Act pre-synaptically: 2) Generalized tonic-clonic seizures CNS: Diplopia, Ataxia ,drowsiness, unsteadiness.
to  synaptic 3) Trigeminalneuralgia. GIT: Vomiting , Diarrhoea.
transmission. 4) Mania. H2O retention & hyponatremia.
Old Drugs

 Inhibit uptake & release of NE. 5) Diabetes Insipidus (DI). IDIOSYNACRATIC BLOOD DYSCRASIS
Aplastic anemia
Agranulocytosis.
Leucopenia.
Hepatic dysfunction.
TERATOGENECITY
Fetal malformation ( neural tube defects).
valporate doubles teratogenicity.
Na Valporate NOT used during PREGNANCY .  Inhibite GABA aminotransferase 1) Partial seizures. DOSE DEPENDENT
to  GABA conc. 2) Generalized seizures: Nausea, vomiting, abdominal pain.
 Block Na-voltage channels. a.tonic-clonic. Weight gain, ↑ appetite.
b.absence. hair loss, fine tremor.
c. myoclonic. IDIOSYNATRICREACTION
3) Bipolar disorder(mania). Hepatotoxicity.
4) Migrineprophylaxis. Thrombocytopenia.
Pancreatitis.
TERATOGENECITY
Spina bifida,Cardiovascular abnormality.
Orofacial & digital abnormalities.
Penobarbital It is well tolerated, with single dose  Enahancement of GABAergic 1) Partial seizures Drowsiness , lethargy , depression
Barbiturates

Mephbarbital Contraindication. pathway. 2) Generalized tonic-clonic seizures. Nystagmus,ataxia.


Metabarbital o Porphyria (acute attack may occur)  Reduction of Glutamate action. 3) Status epilepticus. Memory loss, irritability & mental confusion.
Primidone is used in treatment of  Block Na & Ca(L,N) channels. 4) Febrile convulsion Teratogenic & hemorrhagic disease of new born.
Primidone Essential Tremor resistant to Megaloblastic anemia & osteomalacia.
PROPRANOLOL. Tolerated with single dose.
P H R M A C O L O G Y - NOTE 14 - Treatment of Epilepsy
 Partial seizures& generalized tonic-clonic;cont…Ϳ
DRUG PHARMACOKINETIC MECHANISM OF ACTION USES SIDE EFFECT
Lamotrigine Block Na-voltage channels, adjunctive therapy for refractory: Dizziness, nausea & headache.
to stabilize pre-synaptic o Partial seizures. Diplopia.
neuronal membranes. o 1o & 2o generalized tonic-clonic Somnolence.
reduces the release of excitatory seizures. Skin rash.
amino acids (Glutamate & Aspertate) Flu like symptoms.
Gabapentine It is an analogue of GABA .  GABA synthesis & release. 1) Resistant partial seizures. Somnolence.
It crosses blood brain barrier. block L type Ca channels. 2) Resistant generalized tonic-clonic. Dizziness & headache.
Agonize GABABreceptor. 3) Bipolar disorders. Ataxia & tremors.
4) Migraine and neuropathic pain.
Vigabatrine 
GABA conc. by 1) Partial seizures. NOT AT TOXIC DOSE
irreversible inhibition of 2) 2o generalized responsible by Dizziness, drowsiness.
GABA aminotransferase. seizures. other drugs Weight gain.
3)Infantile spasms. Agitation, confusion & psychosis.
LONG USE
Irreversible Visual field defects.
Topiramate NOT used during PREGNANCY . Enahancement of GABAergic pathway. adjunctive therapy for refractory: Somnolence, fatigue & Dizziness.
Newer Drugs

Block Na-voltage channels. o Partial seizures. Nervousness & confusion.


Block or antagonize Glutamate o Generalizedtonic-clonic Acute myopia ,glaucoma & urolithiasis.
receptors (weak). seizures. Teratogenic abnormalities.
Tiagabine Treatment by discontinuous doses prolongs the inhibitory action of adjunctive therapy for partial Nervousness, confusion.
prevent : synaptically released GABA. seizures. Difficulty in concentration & depression.
Excessive confusion. Tremor & ataxia.
Somnolence. somnolence & dizziness.
Ataxia.
Zonisamide  Block Na channels. 1) Partial seizures. Drowsiness.
Block Ca-voltage channels. 2) Generalised tonic-clonic seizures. cognitiveimpairment.
3)Infantile spasms & myoclonas. Serious skin rashes.
Levetriacetam  At brain-specific binding site, it affects: adjunctive therapy for partial Asthenia.
GABA receptors ( sensitivity) seizures Dizziness.
Ca-voltage channels (block). with or without Drowsiness.
K-channels. generalization.
Felbamate  block NMDA receptor via GLYCINE Refractory partial & generalized Insomnia.
binding site. seizures(3rd line). Dizziness.
resistant seizures as in Lennox- Ataxia.
Gastaur syndrome. Aplastic anemia.
Sever hepatitis.

LENNOX-GASTAURE SYNDROM
It consiste of:
multiple seizure types.
mentalretardation.
refractoriness to anti-seizure drugs.
P H R M A C O L O G Y - NOTE 14 - Treatment of Epilepsy
 Generalized tonic-clonic
DRUG PHARMACOKINETIC MECHANISM OF ACTION USES SIDE EFFECT
Ethosuximide Therapeutic levels & Dosage– 60-100 Inhibits: Absence seizures GIT:
mg/ml achieved with 750-1500mg/day. T type Ca-channels in thalamas. Pain, nausea & vomiting.
It depresses the cerebral MR. Na/K ATPase. CNS:
The clearance is reduced by Valporic GABA aminotransferase enzymes Headache, dizziness, euphoria
Acid. It depresses the cerebral MR. Blood:
Eosinophilia.
Pancytopenia (Thrombocytopenia, leucopenia)
Transient lethargy or fatigue.
Skin rash.
Steven Johnson syndrome.
SLE.
Trimethadone NOT used during pregnancy. Petit mal epilepsy ( drug of choice). Sedation.
Act actively against Pentyleneterazole HEMERALOPIA(reversible impaired visual
that induce seizures. adaptation)
 Others
DRUG PHARMACOKINETIC MECHANISM OF ACTION USES SIDE EFFECT
Diazepam used I.V. or rectally They act as anti-epileptic by: Generalized tonic-clonic (grand-mal). Sedation. 
 GABAergic activity. Status epilacticus Tolerance.
Lorazepam longer acting than diazepam. CLORAZEPATE More effective in status epilepticus. paradoxicalhyperactivity(in 
Benzodiazepines

Clonazepam DIPOTASSIUM---Used as an. Absence (petit mal) siezures. children). 


are common adverse effects. Myoclonicseizures. Ataxia, hypotonia , dysarthria. 
Nitrazepam Less potent than Clonazepam.
CLOBAZAM— infantile spasms. Salivation.
ADVERSE effects of ↑respiratorLJ secretions.
Clorazepate adjunct to treatment of complex Drowsiness.
Benzodiazepins ------ partial seizures.
Dipotassium Lethargy.
 . WITHDRAWAL SYMPTOMS
Clobazam Commonly not used due to quick & high less sedative.
Exacerbation of seizures if
tolerance High TOLERANCE
the drug is stopped suddenly.
Acetazolamide It is a carbonic anhydrase inhibitor Exerts its anti- seizure activity by: Epilepsy during menses (as it Tolerance (quick develop).
Mild acidosis in the brain. discontinuously administrated, NO
rolerance)
Sulthium It is a carbonic anhydrase inhibitor

TYPE DRUG OF CHOICE ALTERNATIVE DRUG

Ethosuximide
Lamotrigine

Phenobarbito
ALTERNATIVE

Phenobarbiton

Gabapentine
Clonazepam
Clonazepam
Simple partial Phenytoin Gabapentine

Lamotrigine
Lamotrigine

Vigabatrine
Topiramate

Topiramate
DRUG

Felbamate
Phenytoin
GENERALIZEDSEIZURES

Phenobarbiton Clobazam

Tiagabine
Complex partial Phenobarbitone Felbamate
SEIZUREs
SIMPLE

Partial with secondarily valporate Topiramate


generalised Lamotrigine Tiagabine
Phenytoin Gabapentine

Ethosuximide

Carbamazepi
Clonazepam
Clonazepam

Lamotrigine
DRUG OF
CHOICE

Primidone
Phenytoin
Valporate

Valporate

Valporate

Valporate
Type Absence Atonic Myoclonic Grand mal/tonic/clonic
P H R M A C O L O G Y - NOTE 15 – Anit-migraine Drugs
ANTI-MIGRINE DRUGS

Acute Attack Prophylaxis

Mild to Moderat to β adrenergic Ca channel 5-HT2 5HT2 antagonist


Moderate Specific drug blockers Other
Sever blockers antagonist /partialagonist

P Agonest for α-
NSAIDs Anti- emetics prokinetic Diclofenac 5-HT Agonist Adrenceptors & 5- Propranolol Flunarizine Pizotifen Methysergide Amitryptyline
HT R

Diphenhydr- Metocloper- Cyprohepata-


Aspirin Sumatripan Ergotamine Metoprolol Nicardipine Imipramine
amine amide dine

Paracetamol Promethazine Domperidone Almotriptan Nadolol Nifedipine Sertraline

Ibuprofen Naratriptan Atenolol Nimodipine Fluoxetine

Indomethacin Pizatriptan Timolol Verapamil Clonidine

Naproxene Zolmitriptan Valporate

Opioids
P H R M A C O L O G Y - NOTE 15 – Anit-migraine Drugs
 Acute attack of Migraine
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Aspirin  Given orally. Analgesic. acute migraine attack.
Mild to Moderate

Paracetamol they must be given early to be absorbed


NSAIDs

Ibuprofen before there is vomiting.


attack

Indomethacin
Naproxene
Opioids Given parentrally (I.V. or I.M.). Refractory cases of
acute attack of
Efficient use of analgesic &
migraine(rarly)
antiemetic is sufficient for the
Diphenhydramine Prevent vomiting.
majority of ACUTE ATTACKS
Anti- emetics
Moderat to Sever

Promethazine
attack

Metocloperamide Given by I.V. injection. They promote gastric emptying, With very severe
prokinetic

So, enhances absorption of vomiting.


Domperidone Given as rectal suppositories for vomiting can analgesics.
be tried
Diclofenac
Sumatripan Given by oral route or S.C. injection. stimulate 5-HT1 R on pre- acute severe migraine Malaise ,fatigue.
Fast absorbtion. synaptic endings of V cn. attack(1st line). Sedation.
Bioavailabilty by s.c. route is 96% inhibit releasing of Dizziness, vertigo, nausea & vomiting.
Dose not cross BBB. vasodilators . NOT used with feeling of chest pressure, tightness & pain.
5-HT Agonist

Plasma t1/2 is 2 hours. selectively stimulates IHD. CARDIAC ARRHYTHMIA & myocardial infarction.
5HT1B/1D R in cranial BV, unstable angina.
due to coronary artery spasm.
constrict them. previous MI
Almotriptan they are congeners of Sumatriptan. Less side effects.
Specific drug for acute attake

+ effects
on CNS
Naratriptan improved pharmacokinetic Reduce cardiac side effects.
Pizatriptan better Bioavailability.
better and longer duration.
Zolmitriptan
Ergotamine Ergotamine tartrate stimulate 5-HT1 R on pre-synaptic Migrine (high specific). Paresthesiae in hands & feet.
Given by o Entral route (oral, sublingual, rectal). endings of V cn. Peripheral ischaemia.
P Agonest for α-Adrenceptors & 5-HT R

o Parentral route (inhaler). inhibit releasing of Peripheral GANGRENE with overdose.


rectal route is preferred ???. vasodilators . Precipitate angina pectoris.
caffeine facilitates absorption of ergot alkaloid. Fetal damage.
It metabolized in the liver.
t ½ is 2 hrs
NOT used with disease
DOSE. of:
o Tablet (1mg + Caffeine 100mg). Coronary BV.
o 1-2 tab. at onset ,then 1 tab/ 30min. Peripheral BV.
o NO > 6 mg/attack & NO >10 mg/wk.
For severe attack, it ginen may be IM/IV injct.
Dihydroergotamine oFor intractable migraine.
oGiven by IV inj.(0.5-1mg)
P H R M A C O L O G Y - NOTE 15 – Anit-migraine Drugs
 Prophylaxis drugs for Migrine.
DRUG PHARMACOKINETIC ACTION USES SIDE EFFECT
Propranolol • PROPRANOLOL– (effect , the d-isomer part of structure lacks β They are effective and widely used. Fatigue.
also prevent migraine ). blocking action; Broncho-constriction.
β adrenergic blockers

Alter the permeability of the


membrane.
Metoprolol
Nadolol
Atenolol
Timolol
Block Ca channel. effective in the preventive treatment 
Ca channel blockers

Flunarizine
Nicardipine of Migraine
Nifedipine
Nimodipine
Verapamil
Pizotifen antagonize5-HT2 receptors. They are RARELY used Weight gain.
antagonist

Atropine like action. Anti-cholinergic side effects.


5-HT2

Cyprohepatadine Antagonize 5-HT2 R & H 1 R. Sedation.


Block Ca channels weight gain.
Methysergide effective in about 60% patients. It is 5HT2 antagonist /partial agonist Serious Toxicities like;
5HT2 antagonist
/partial agonist

o RETROPERITONEAL
obstruction to the Ureters.
o Subendocardial, Pericardial or Pleural fibrosis.
Nausea, vomiting & diarrhoea.
Amitryptyline effective for the PROPHYLAXIS of
Imipramine migraine in some patients.
Other

Sertraline
Fluoxetine
Clonidine
Valporate