Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Direct Cholinergic Agonists

Note: Do not use if
Bowel obstruction,
Asthma, Peritonitis
Muscarine Muscarinic No CNS action

Nicotine Nicotinic

Pilocarpine Pred. Muscarinic Glaucoma, Xerostomia

Bethanechol Pred. Muscarinic Stimulate Bladder, GI, Longer duration

Paralytic ileus

Carbachol Pred. Nicotinic Open-angle Glaucoma

Cevimeline Muscarinic Xerostomia, Dry eyes Sjogren's syndrome

Indirect Cholinergic Agonists (reversible)

Note: Do not use if
Bowel obstruction,
Diagnostic for Asthma, Peritonitis Neostigmine analog with
Edrophonium Cholinergic Crisis shorter duration

Neostigmine Myasthenia Gravis,

Urinary retention, etc
Excess can cause
Physostigmine Anticholinesterase Glaucoma, CNS Depolarizing
seizures Neuromuscular
Blockade
Pyridostigmine Myasthenia Gravis,
Curariform drug toxicity

Donepezil Possible Alzheimer's Tx Crosses BBB

 Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Indirect Cholinergic Agonists (irreversible)

Note: Do not use if
Bowel obstruction,
Asthma, Peritonitis Very lipid soluble,
Isoflurophate (DFP) Glaucoma (long-term) Duration is >1 week

Echothiophate Organophosphate cov- Glaucoma Duration is >1 week

alent bond w/ Esterase

Malathion Pediculosis (lice) Mammals can inactivate,

Insects can't (pesticide)
Nerve Gas (Soman, Phosphorylated
Esterase that cannot None
Pralidoxime (2-PAM)
can help if early (No
Tabun, VX) regenerate CNS)

Acetylcholine Augmenters

Sildenafil (Viagra) Differences due to

Headache, nasal duration of action;
Inhibit 5-PDE, increase Metabolized by
congestion, dyspepsia, CYP3A4;
Tadalafil (Cialis) cGMP --> Vasodilation Erectile dysfunction visual disturbances (blue used withShould not be
vision w/ Viagra) Nitrates or
other PDE blockers ->
Vardenafil (Levitra) hypotension

Cholinergic Antagonists (Antimuscarinics)

Atropine Eye dilation Aggravates Glaucoma

Scopolamine Motion sickness; CNS probs: euphoria, Greater CNS effects

mydriasis, cycloplegia restlessness, delerium than Atropine

Homatropine Muscarinic competitor Short duration, synthetic

blocks M1, M2, and M3
 Muscarinic competitor
blocks M1, M2, and M3

Propantheline Synthetic

Ipratropium Inhalation Less due to minimal lung Local action taken as

Bronchodialator absorption mist, Synthetic

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Pirenzipine Blocks M1 in ganglia

Dicyclomine Blocks M3 in parietal Ulcers (oldfashioned),

cells relaxing smooth muscle

Tolterodine (Detrol) Blocks

Bladder
M2 and M3 in Hyperactive bladder more selective to
bladder

Cholinergic Antagonists (Antinicotinics-Ganglionic blockers)

Hexamethonium Emergency HTN crisis

Pentolinium Block both

Non-depolarizing Parasympathetic and
blockade of NG receptor Sympathetic…Effects
depend on dominant
Trimethaphan Emergency HTN crisis tone short half-life

Mecamylamine

Cholinergic Antagonists (Antinicotinics-Neuromuscular Junction blockers)

Tubocurarine Given IV or IM

Pancuronium
Non-depolarizing Some association with
blockade of Nnmj receptor Histamine release due to
Mivacurium Muscle relaxation large size
Competes with Ach at before and during (bronchospasm and
receptor surgery, ECT, Tetanus edema)
convulsions, orthopedic
procedures
 Non-depolarizing Some association with
blockade of Nnmj receptor Histamine release due to
Muscle relaxation large size
Competes with Ach at before and during (bronchospasm and
receptor surgery, ECT, Tetanus edema)
convulsions, orthopedic Seizures due to
Atracurium procedures metabolites in CNS

Vecuronium Excreted by liver (used

in Pts with renal probs)
Depolarizing blockade of
Succinylcholine Nnmj receptor Malignant hyperthermia Contract then paralyzed
(Pseudocholinesterase)

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Other "Muscle Relaxers"

Dantrolene Unknown; Decreases Malignant hyperthermia Hepatotoxicity

Ca release from SR

Botulinum toxin Blocks Ach vesicle Prevent sweating,

release (for months) cosmetic
Black Widow Spider Massive release of Ach
Venom from vesicles

Direct Adrenergic Agonists (Sympathomimetics)

Epinephrine Low dose: B (dilation) Asthma, anaphylactic CNS effects (tremors, All adrenergic receptors
High dose: a (constrict) shock, glaucoma stroke), arrhythmias

Norepinephrine Beta 1 and alpha Shock, but decrease in All receptors but Beta 2
RBF
Low dose: B1 (D1, D2) Shock-inc. CO w/ maint
Dopamine of renal blood flow
High dose: a

Dobutamine Beta 1 (some Alpha) Increase CO in CHF

Phenylephrine Alpha 1 >> Alpha 2 topical, eye, nasal reflex bradycardia

decongestant

Methoxamine Alpha 1 Paroxysmal supravent. Does not stimulate heart

tachycardia

Metaproterenol Beta 2 Bronchodilator Similar to Albuterol,

Ritodrine, Terbutaline
Isoproterenol Beta 1 and Beta 2

Clonidine Alpha 2 (in CNS) Control of BZ and opiate Inhibits sympathetic

withdrawl vasomotor centers

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Indirect Adrenergic Agonists

Amphetamine Beta 1 and alpha

mediates Norepi release

Tyramine causes release of Metabolized by MAO

Norepi (careful with inhibitors)

Cocaine Beta 1 and alpha Local anesthetic activity Peripheral and CNS
blocks Reuptake 1 with analogs blocks reuptake of effects
Dopamine and Norepi
Cardiac death from
build-up of Norepi

Mixed Adrenergic Agonists

Ephedrine
Direct: a and B
Indirect: release of Viral and allergic rhinitis Can cause HTN crisis
Norepi
Pseudoephedrine

Metaraminol Direct: a Indirect: Hypotensive states No CNS-too polar

rel. of Norepi

Alpha-Adrenergic Antagonists

Phenoxybenzamine Pheochromocytoma orthostatic hypotension Decreases TPR and

blood pressure
Non-selective alpha
blocker
 Non-selective alpha
blocker
Phentolamine reflex tachycardia can
worsen heart condition

Doxazosin

Tamsulosin Decreases TPR and

Selective Alpha 1 hypertension, urinary nasal congestion, blood pressure
blocker retention due to BPH orthostatic hypotension, Little effect on CO or
first dose syncope RBF
Alfuzosin

Prazosin

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Beta-Adrenergic Antagonists

Propranolol Bronchoconstriction,
HTN, glaucoma, arrhythmias at withdrawl
migraine, CV, thyroid,
Non-selective beta stage fright
Nadolol blocker longer duration

Timolol Topical for glaucoma

Atenolol HTN with impaired Will not block B2 (no

pulmonary function added lung problems)
Selective Beta 1 blocker
Metoprolol

Agents with Intrinsic Sympathomimetic Activity

Pindolol, Acebutolol Not pure B antagonists

Partial agonists
HTN in Pts who cannot
tolerate increased TPR

Beta and Alpha 1 Antagonists

Labetatol HTN in Pts who cannot Inhibits vasoconstriction
tolerate increased TPR of pure B blockers
Blocks B and a1
Carvedilol HTN, MI; heart failure Antioxidant and
Antiapoptotic activity

Other Agents with Adrenergic Agonistic Activity

Reserpine inhibits storage of Depletes Norepi with

Norepi in vesicles decrease in sympathetic

Guanethidine blocks release of stored

Norepi

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Local Anesthetics

Procaine Short-acting, Ester

(PABA metabolites)

Lidocaine CV, CNS depression, Intermediate-acting

Blockade of Na+ channel Anesthetic…
fibers, then
blocks C-
Adelta-
Antiarrhythmic
in membrane… prevents fibers, then Aalpha
depolarization motor fibers
Bupivacaine Long-acting

Benzocaine Topical only

Other Agents with Na+ Action

Tetrodotoxin Puffer fish poison

Binds near Na channel
Blocks opening
Saxitoxin Red tide

Scorpion Venom Binds within channel

Prevents inactivation
General Anesthetics

Nitrous Oxide Surgery, Recreational Minor CV, resp and SM Gas, rapid onset and
(Whip-its) effects, CNS toxicity recovery (low lipophilic)

Halothane Blunts resp, CV, uterus, No analgesic effect,

Malignant hyperthermia reactve metabltes->Hep
Surgery
Isoflurane Ion channels, signal Greater Resp. Used a lot, not good with
transduction depression, bad odor longer procedures

Methoxyflurane Labor and delivery Analgesics, not much Most potent of gas
uteran; Nephrotoxicity agents

Sevoflurane Surgery little CV or organ toxicity limited metabolism

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Thiopental GABA receptors CNS Depression Resp and CV toxicity Induction Agent
(anesthetic)
Midazolam, Valium Potentiation of GABA Conscious sedation with Countered with
(Benzodiazepines) (inhibitory effects) amnesia Flumazenil

Propofol Induction (replaced Decreased TPR

Thiopental)

Ethomidate Hypnotic Vomiting, Nausea, pain No analgesic effects

on injection

Fentanyl (Opiods) Analgesia w/ amnesia Less CV effects Replaced morphine and

meperidine

Ketamine NMDA antagonist Catatonia without CV or Similar to PCP: weird Dissociative anesthetic
Resp depression dreams/visions, inc ICP

Drugs for Parkinson's (loss of DA action)

Coenzyme Q10 Can slow progression

Levodopa (L-Dopa) Converted to Dopamine Parkinson's Disease Similar to DA (but less) Large first-pass, to CNS
by ACTIVE transport
Carbidopa Blocks AAAD in Periph. Lessens peripherals, Does NOT cross BBB
More L-Dopa in CNS may increase CNS ones (prevents --> DA in Per.)

Selegiline (deprenyl) Inhibits MAO type B Preventing DA Adrenergic stimulation Type B more specific to
metabolism DA at small doses

Entacapone Inhibits COMT NO hepatotoxicity

Prevent DA metabolism
and allow more L-Dopa
to enter CNS
Tolcapone Inhibits COMT Hepatotoxicity Not used much anymore

Bromocriptine
Still active at later
stages when DA For all DAergic drugs:
neurons completely lost Per - arrythmias (B1),
Pergolide hypotension
Dopaminergic agonists CNS -N/V(emetic center) Cross BBB
dyskinesias, agitation,
Pramipexole hallucinations (DA
receptors in other parts
of brain)
Ropinirole

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Other Drugs for Parkinson's

Benztropine
Anticholinergic agents Reduce excitation of Muscarinic blockade:
GABA neurons Can't see,spit,pee,shit
Trihexyphenidyl

Amantadine Synthesis, release, Antiviral, seemingly Livedo reticularis (bluish

reuptake of DA? helpful for PD skin w/ edema)

Amphetamine Blocks reuptake of DA

Parkinson's Drug Interactions

Antipsychotic drugs DA-receptor antagonists Can worsen PD Can lower effectiveness

symptoms of PD drugs
Pyridoxine (Vit. B6) Co-factor
metabolism
for L-Dopa Supplementation can
decrease [L-Dopa]

Tyramine Increases levels of NE, HTN crisis --> Death MAO inhibitors can
can also act directly prevent breakdown

Drugs for Hyperkinetic Disorders (loss of GABA action)

Reserpine
Huntington's Chorea Do not work very well
Antipsychotics
Tetrabenazine (Dopamine Tardive Dyskinesia
antagonists/depletors)
Haloperidol Tics (Tourette's)

Clozapine Atypical antipsychotic Does NOT cause

Tardive Dyskinesia

Propranolol Nonselective Beta Tremors

Blocker

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Drugs for Psychiatric Disorders (Antipsychotics)

D2 blockers Block DA type 2 Positive symptoms Blockade of DA's in

receptors (delusions, craziness) Usually safe, unless other parts of brain, or
combined (EtOH), other receptors
5HT2 blockers Block 5-HT type 2 Negative symptoms increased Prolactin with (Ach,His) can lead to
receptors (anergy, depression) DA blockade, TD, side effects
Antipsychotic malignant
syndrome
Phenothiazines

Chlorpromazine Also antiemetic, First antipsychotic drug

antihiccup

Thioridazine Arrhythmias w/ overdose High sedation, alpha-

Pigmentary retinopathy blockade, Low EPS

Fluphenazine Depot preparation for

compliance probs

Classical antipsychotics
- Reduce dopamine
action
Perphenazine
Classical antipsychotics
Prochlorperazine - Reduce dopamine
action
Thioxanthines

Thiothixene

Butyrophenones

Haloperidol Most widely used of Low sedation, alpha- Depot preparation for
classical antipsychotics blockade, High EPS compliance probs

Heterocyclic (newer agents)

Clozapine Requires WBC Agranulocytosis, Increased antimuscarinic

monitoring Low EPS/TD Low Prolactin elevation
Low D1, Moderate D2, EPS at high doses, More
Risperidone High D4, High 5-HT2 Prolactin elevation
Similar to Clozapine Do not require WBC
monitoring
Olanzapine Very low agranulocytosis

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Bi-Polar disorder Fatigue, hand tremor Behaves similarly to Na+

Most likely interferes Neph. diabetes insipidus Compete 4 reabsorption
Lithium with IP3 and DAG paths
(Manic phase, mood Very small TI - CNS No tolerance to tremor
swings, antidepressant) toxicity (coma, others) or diabetes insipidus

Antiepileptic Drugs Possible birth defects, Also used for pain control, diabetic neuropathies,
OC interactions and withdrawl symptoms control

Carbamazepine Like Phenytoin; + DOC Drowsiness, vertigo,

for Trigeminal Neuralgia ataxia NOT used for Absence
(petit mal) seizures;
Block Na+ channels in Tonic-clonic (GM), Gingival hyperplasia, zero-order at [high]
Phenytoin (1o) brain; reduce neuron Psychomotor, and Focal nystagms,atxia,hirsutsm
firing
 Block Na+ channels in
brain; reduce neuron
firing
Fosphenytoin More hydrophilic IM/IV;
In ER for FAST action
Valproic acid (2o) Prolongs GABA, Blocks Anticonvulsant and Liver failure in kids
(Valproate) Na+ and T-type Ca2+ mood-stabilizer (with overdose)

Phenobarbital GM, Psychomotor, and Sedation or hyperactivity Least toxic; --> Children
Focal; also (EtOH w/x) to avoid gum growth
Metabolized to Allows for greater activity with less blood levels of
Primidone Phenobarbitol and Myoclonic in children Phenobarbital, therefore less sedation
PEMA
Ethosuximide (1o) Blocks T-type Ca2+ Absence (petit mal) Extended depression Contra in tonic-clonics
channels ONLY -- usually children (GI, drowsiness, lazy)

Clonazepam Stimulates GABA Useful in all, esp. Drowsiness, ataxia, Potential to exacerbate
myoclonic and akinetic aggressiveness seizures; yes Tolerance

Diazepam Status epilepticus Medical emergency

Therapeutic Adjuncts (some can be used alone)

Clorazepate Converted to Diazepam Prodrug

Felbamate Blocks NMDA? Partial sz in Adults Aplastic anemia, GI, and 0-order, increases
Potentiates GABA? CNS [valproate,phenytoin]

Gabapentine Increase GABA Partial sz; Pain control -

release? (more common use)

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Lamotrigine Inactivates Na+ channels Partials, some GM, Cerebellar dys, Possibly leading to
atonic, and absence drowsiness, and rash Stevens-Johnson syn.

Topiramate Blocks Na+ channels, Partial sz (approved for Ataxia, drowsiness Also inhibits glutamate
augments GABA monothrpy), migraines at certain receptors

Vigabatrin Irreversible inhibitor of Complex Partial sz Psychotic rxns, Not available in USA
GABA transaminase (Psychomotor) hyperactivity

Levetiracetam Partial sz

Zonisamide Partial sz Newer agents

 Newer agents

Tiagabine Blocks GABA reuptake Partial sz

Lorazepam Another option for

status epilepticus

Opioid Agonists Presynapse: close Ca2+ Effects of receptors (Mu,

Postsynapse: open K+ Delta, Kappa)

Histamine release due to

Analgesia (Mu), Resp. depression, large size; Pharmaco-
Morphine Stimulation of Mu, Diarrhea, Cough, Sedation, Constipation, dynamic tolerance 2-3
kappa receptors Surgery Nausea/vomiting (CNS), wks; High dependence;
Addiction Changed to M-3-G (les)
and M-6-G (more active)

Meperidine Mild to moderate pain; Neurotoxicity, seizures No cough suppression,

Avoid chronic use from metabolite NO miosis (abuse!)

Methadone Withdrawl from heroin Less euphoria, slow Slower onset, longer
or morphine withdrawl duration of action

Fentanyl Anesthesia (sedative, 80x better analgesic Transdermal form -

analgesic) potency than morphine slower onset, long DOA

Codeine Metabolized in liver to Cough, Pain relief (w/ Some people lack
Decreased dependence CYP2D6
morphine by CYP2D6 NSAIDs) (no pain relief)
Oxycodone, Mild-moderate agonists Pain control
Hydrocodone

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Propoxyphene Derivative of Methadone Weak analgesic Cardiotoxic, Pulmonary No benefit over other
edema drugs; use declining

Pentazocine Partial agonist (Mu, Analgesia (kappa) Withdrawl sx when given Talwin-NX to prevent IV
delta, sigma) with morphine abuse

Opioid Antagonists
Naloxone Opioid toxicity (Resp. Can try in ER with Talwin-NX (no
depression, coma) comatose pt. absorption orally)
Pure antagonist (mainly
at Mu receptors)
Naltrexone Opioid, EtOH addiction Longer onset, T1/2,
duration of action

Sedative-Hypnotic and Anxiolytic Drugs

Barbiturates Tolerance --> Smaller

Therapeutic index

Phenobarbital
Enhances duration
GABA binding to Longer-acting Can produce anesthesia
receptor --> Cl- influx --> Primarily for and even death;
Pentobarbital hyperpolarization anticonvulsants/ Withdrawl sx can be
(Can affect Cl- anesthetics fatal
conductance w/o GABA) Very short-acting (lipid
Thiopental soluble-->redistribution)

Miscellaneous

Buspirone Partial agonist at 5- Anxiety only Does not interact with 1-4 weeks to start
HT1a receptors EtOH, motor skills working

Propanolol Non-selective beta Chronic anxiety, panic Contra: Diabetics,

blocker attacks asthmatics
Zolpidem (Ambien), Selective for BZ1 Hypnotic similar to BZ's Less tolerance,
Zaleplon receptor (sleep) dependency, amnesia

Chloral hydrate Rapid onset, short Low TI Unpleasant taset/smell

duration

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

BZ1 = sleep, BZ2 = Anterograde amnesia, Will NOT produce

Benzodiazepines few outside of CNS anesthesia or death
memory/motor function

Alprazolam All of these can cross

placenta --> probs.

Chlordiazepoxide All these only toxic when

combined (EtOH)

Varied: some Overdose similar to

anticonvulsants, muscle EtOH intoxication;
Enhances frequency relaxors in addition to
GABA binding to anxiolytic/sedative/ all can develop
receptor --> Cl- influx hypnotics dependence
resulting in
hyperpolarizatioin
Clonazepam Varied: some Overdose similar to
anticonvulsants, muscle EtOH intoxication;
Enhances frequency relaxors in addition to
GABA binding to anxiolytic/sedative/ all can develop
Diazepam (Valium) receptor --> Cl- influx hypnotics dependence Oral form for kids
resulting in
hyperpolarizatioin
Lorazepam (inhibitory effect in brain)
GABA must be present
Oxazepam to show any effect
(cannot affect Cl-
conductance alone)
Flurazepam Daytime sedation, Long-acting active
Nightmares metabolite
For staying asleep
Temazepam

Triazolam For starting sleep Daytime anxiety, Shorter-acting

morning insomnia

Flumazenil BZ receptor antagonist Hasten recovery, Also antagonizes

overdose zolpidem and zaleplon

Drugs for Depression Also used for Panic disorder, Enuresis, Chronic No CNS stimulation for
pain, Eating disorders, Attention Deficit disorder normal patients

Monoamine Oxidase Inhibitors Nasty drugs MAOa = NE, 5-HT

MAOb = DA

Phenelzine
Low TI; hypotension, Hepatotoxicity
Increase vesicular sexual dysfunction,
Isocarboxazid stores of NE and 5-HT insomnia, OD sx's,
Tyramine crisis,
potentiates meperidine
Tranylcypromine

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Tricyclic Antidepressants

Amitriptyline Higher incidence of

anticholinergic
Very low TI; OD can be
fatal (treat symptoms);
potentiate
amphetamines (block
Block reuptake of 5-HT reuptake); counter
and NE Guanethidine and
Clonidine (HTN), and L-
dopa due to delayed
 Very low TI; OD can be
Clomipramine fatal (treat symptoms);
potentiate
Similar to antipsychotics amphetamines (block
Desipramine Block reuptake of 5-HT (block alpha, histamine, reuptake); counter
and NE muscarinic receptors) Guanethidine and
BUT don't block DA Clonidine (HTN), and L-
receptors dopa due to delayed
Imipramine (so you see arrythmias, gastric emptying
constipation, seizures) (antimuscarinic)
Nortriptyline

Selective Serotonin Reuptake Inhibitors High TI (death only with Requires downregulation
combos) of autoreceptor 4 activity
Long T1/2 of metabolite
Fluoxetine (Prozac)
(least w/x sx)
CNS stimulation, sexual
Fluvoxamine dysfunction; inhibition
Block reuptake of 5-HT of P-450 (esp.
selectively fluoxetine, paroxetine);
Serotonin syndrome
Paroxetine (esp. w/
MAOIs/meperidine)
Sertraline (Zoloft)

Other Antidepressants

Bupropion

Mirtazapine Inhibits presynaptic

alpha 2 receptors

Trazodone Blocks reuptake of 5-HT

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Venlafaxine Inhibits reuptake of NE

and 5-HT
Nefazodone

Maprotiline Inhibits reuptake of NE

Hypothalamic-Pituitary Drugs

Bromocriptine Excess Prolactin

Block prolactin (and GH)
production
Cabergoline Excess Prolactin and Long-acting; DA agonist
GH
Chorionic Can induce ovulation,
gonadotropin (hCG) Acts like LH steroidogenesis

Gonadorelin (GnRH) Stimulates

when pulsed
LH/FSH Diagnostic tool - locate
problem of HP-axis
Inhibit LH/FSH if given
Too much E2/Test. - Endometriosis, uterine continuously
Leuprolide (Leupron) Long-acting GnRH
agonist (less LH/FSH) fibroids, precocious puberty, prostate cancer

Menotropins (hMG) Mostly FSH (some LH) In Vitro clinics From urine of
postmenopausal women

Octreotide Blocks GH production

(acts like somatostatin)

Sermorelin (GHRH) Stimulates GH

production by pituitary
Diagnostic tool - can
they make GH?

Somatropin GH analog By recombinant DNA

Abarelix GnRH receptor Prostate cancer

antagonist

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Thyroid Drugs

Levothyroxine (T4) Stimulates cellular Hypothyroid Long T1/2 (7 days)

metabolism when -->T3 (Hashimoto, Lithium)
Propylthiouracil Blocks organif. of I and Hyperthyroid (Graves) Can cross placenta Inhibits thyroid hormone
(PTU) coupling of iodotyrosine synthesis (not I uptake)

Adrenal Drugs/Hormones Mostly Non-adrenal

Hydrocortisol Glucocorticoid Cannot bind to aldosterone receptor due to

(cortisol) actions of 11beta-HSD-2 --> cortisone (inactive)

Cortisone Converted to cortisol

(11beta-HSD-1) Many uses
(Hypofxn=Addison's,
fetal lung maturation)
Betamethasone Adrenal suppression Long-acting; Only have
(must taper drugs when glucocorticoid effects;
discontinuing), used to test axis
Dexamethasone hyperglycemia,
hypertension/Na
retention, edema,
Prednisolone Synthetic Acts like cortisol Iatrogenic Cushings
glucocorticoids

Prednisone Converted to Intermediate-acting

Prednisolone

Triamcinolone

Fludrocortisone Synthetic 20x more mineralC. vs.

mineralocorticoid glucoC. effects
Mifepristone Binds to glucocorticoid, Cushing Syn., Postcoital Antagonist
(RU-486) progesterone receptors contraceptive
 Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Gonadal Drugs/Hormones

Tamoxifen Selective estrogen Binds to receptor

receptor modulator
Breast cancer
Anastrozole
Aromatase inhibitors
Letrozole

Clomiphene Ovulating inducing Ovulation for ppl with

agent polycystic ovarian dis.

Finasteride Blocks 5alpha-reductase

Prostate cancer
Flutamide Androgen receptor
antagonist

Raloxifene Selective estrogen Prevent bone loss Acts only on bone

receptor modulator receptors (not others)

Pancreatic Drugs/Hormones

Insulin Lispro Recombinant insulin

Sulfonylureas (1o) Disulfiram-like rxn

(Glyburide) Act on K+ channel to
make B cell release Type II diabetes
insulin Hypoglycemia, Drug Short-acting; target post-
Repaglinide interactions (EtOH) prandial glucose spikes
Biguanides (1o) Decrease gluconeo- Mainly Type II (if no Glucose enters SM and
(Metformin) genesis, increase usage hepatic/renal disease) adipocytes
Thiazolidinediones Reduces peripheral P450 inducer, edema, Activated PPAR-gamma
(TZD) (Pioglitazone) insulin resistance volume expansion

Acarbose Glucosidase inhibitor - Flatulence

reduces uptake frm gut
 Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Drugs of Abuse

Amphetamine Beta 1, alpha, releases

NE and DA
Methamphetamine
"speed"

Caffeine

Cocaine Blocks DA reuptake CV, psychosis, lowered

(also NE) seizure threshold

Ephedrine

Methylphenidate

Phentermine

Sibutramine
CNS depressant
Ethanol (GABA, Na, NMDA, 5- Social Alcoholic hallucinosis W/drawl CAN be fatal -
HT3???) (DT's), suppressed ADH CV collapse from ANS

Methanol Converted to form- Acidosis, coma, death Treated with EtOH to

aldehyde --> formic acid compete with enzyme

Ketamine

Lysergic acid NO withdrawl syndrome;

diethyl-amide (LSD) Increase in 5-HT activity chemically like 5-HT
Methylene dioxy- CV, "runs", tactile "MDMA", "ecstacy"
CH3 amphetamine hallucinations (worms)

Mescaline Psychedelic NO withdrawl syndrome

Phencyclidine (PCP) Inhibit NMDA channels,
block reuptake DA, NE

Marijuana (THC) G-protein receptor in

CNS

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Dronabinol Cannabinoid (THC) Appetite stimulant, anti-

emetic, anticonvulsant
Heroin (and other Probably involves G- Withdrawl NOT fatal
opioids) protein, cAMP

Nicotine Nicotinic and

dopaminergic pathways

Pentobarbital Barbiturate-general CNS Withdrawl CAN be fatal

depression

Disulfiram Inhibits aldehyde Negative reward for OD can lead to CV Like metronidazole,
dehydrogenase EtOH intake collapse from aldehyde sulfonylureas, cephs, etc

Naltrexone Opioid antagonist

(mainly at mu receptrs)
 Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Thiazide Diuretics "Breaking phenomenon" Some allergies to sulfur

with all Na excretors in structure
Passive Na exchange
distally can --> K loss
Increase LDL, TGs, and
total cholesterol

Hydrochlorothiazide
1o: Blocks NaCl Caution with renal
symporter in early distal HTN (first-line), CHF, insufficiency Rapid onset, relatively
Metazolone convoluted tubule edema, nephrolithiasis, Can --> hypokalemia, short DOA,
2o: Block carbonic diabetes insipidus hyperuricemia, Also DECREASE Ca2+
anhydrase in proximal hypercalcemia, in urine
tubule (weak) metabolic alkalosis
Indapamide

Loop Diuretics (High-Ceiling) Vasodilation following IV

Furosemide

1o: Inhibit Na,K,Cl Hypovolemia,

Ethacrynic acid symporter in thick Edema, acute renal hypokalemia,
ascending limb failure, hypercalcemia, hypocalcemia, Also INCREASE Ca2+
2o: inhibit NaCl chemical intoxication hyperuricemia, in urine
symporter in distal (increases excretion) ototoxicity (esp. E.
Bumetanide acid), impaired platelet
tubule aggregation
Torsemide

Potassium-sparing Diuretics Weak diuretics, usually given with thiazides to

prevent hypokalemia
Amiloride
(more potent) Lack of Na in cell to
Inhibit Na reabsorption hyperkalemia, exchange prevents
in collecting duct CHF (3rd-line), cirrhosis gynecomastia, loss of
w/ ascites, nephritic excretion of K
syndrome, HTN, libido, impotence,
1o aldosteronism menstrual irregularities,
leg cramps
 Inhibit Na reabsorption Lack of Na in cell to
hyperkalemia,
CHF (3rd-line), cirrhosis gynecomastia, exchange prevents
in collecting duct loss of excretion of K
Triamterene w/ ascites, nephritic libido, impotence,
syndrome, HTN, menstrual irregularities,
1o aldosteronism leg cramps
Spironolactone Aldosterone antagonist Also inhibits synthesis of
(mtblzd --> Canrenone) the transporters

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Carbonic Anhydrase Inhibitors Minor diuretics

Acetazolamide Prox. Tubule: Reversibly Glaucoma (main), Fatigue, parasthesias,

inhibit CA --> inhibit epilepsy, salicylate metabolic acidosis, Rapid tolerance
NaHCO3 reabsorption poisoning, acute hypokalemia,
Dorzolamide mountain sickness hyperglycemia

Osmotic Diuretics Minor diuretics

Increase GFR, reduce
eye pressure (eye
Mannitol surgery) intracranial
Prox. Tubule: pressure (neurosurg.), Fatal cellular
Osmotic pull of H2O cerebral edema, toxin dehyrdation (large Filtered at glomerulus,
Pharmacologically inert excretion doses), ionic imbalances minimally reabsorbed
Glycerol

Xanthines

Aminophylline
Increaes GFR, inhibit Na CHF, Cardiac edema (in CNS stimulation, GI Combined with other
reabsorbtion in tubule combination) disturbances diuretics or even digoxin
for CHF, cardiac edema
Caffeine
Anti-Hypertensive Drugs

Diuretics

Hydrochlorothiazide
See above
Furosemide

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Beta-adrenergic Antagonists

Propranolol

Metoprolol Reduce CO, and plasma Cardiosensitive (Beta1)

renin activity; also inhibit Bronchoconstriction
presynaptic beta HTN (except with metoprolol)
receptors, CNS effects,
Nadolol PNS effects

Pindolol

Alpha-adrenergic Antagonists

Prazosin Alpha-1 blocker HTN, BPH Decreases LDL, and

total cholesterol

Inhibitors of Renin-Angiotensin System

Captopril Non-peptide (orally

Renal failure active)
Angiotensin Converting
Enzyme (ACE) inhibitors HTN, CHF, MI, diabetic (reversible), loss of
nephropathy, renal taste, cough, allergy,
insufficiency angioedema,
hyperkalemia, fetal
malformatioin
 Angiotensin Converting Renal failure
Enzyme (ACE) inhibitors HTN, CHF, MI, diabetic (reversible), loss of
Enalapril nephropathy, renal taste, cough, allergy,
insufficiency angioedema,
hyperkalemia, fetal
Angiotensin II receptor malformatioin
Losartan antagonist

Centrally-acting Drugs

Clonidine HTN, insomnia, opiate Decreases LDL, and

w/dx, Tourette's total cholesterol
Alpha-2 agonist:
reduces sympathetics
Methyldopa Preeclampsia

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Vasodilators Combined therapy with diuretics & beta blockers

to prevent adverse reflexes to vasodilators

Diltiazem
HTN, Arrythmias (slow Reflex tachycardia may
Nifedipine Calcium channel blocker conduction through AV worsen heart condition,
node, DECREASE effects on AV conduction
contractility)
Verapamil Avoid in those with
conduction disturbances

Nitroglycerin (IV)
Activation of guanylyl Excessive dilation -->
cyclase --> inc. cGMP Hypotension
Nitroprusside Releases nitric oxide

Minoxidil Activation of ATP-

sensitive K channels

Hydralazine Ca channel blocker, Preeclampsia

inhibits enzymes ->ROS

Fenoldopam Dopamine (D1) agonist Hypokalemia arteriolar dilation, also

afferent AND efferent
Drugs that Alter Hemostasis

Antiplatelet Drugs

Acetylsalicylic acid Irreversible inhibition of

(aspirin) Cyclooxygenase Platelets may be more
Anticoagulation, pain sensitive than vessel
control, antipyretic wall
Ibuprofen (and other Reversible inhibition of
NSAIDs) Cyclooxygenase
Inhb phosphodiesterase Used in combination Potentiates PGI2, inhibts
Dipyridamole --> increased cAMP with aspirin Adenosine uptake
B blocker - inhibits May inhibit TXA2 syn. by
Propranolol platelet aggregation limiting Ca availability

Abciximab Binds to IIb/IIIa During & after coronary Hemorrhage, Monoclonal antibody
adhesion molecule artery procedures thrombocytpenia

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Pentoxifylline Xanthine derivative, Obstructed arteries,

prevents claudication vascular dementia

Ticlopidine
Platelet ADP receptor Anticoagulation in those TTP,
blood
neutropenia, less
cells, increased
antagonist (irreversible) who cannot tolerate LDL, VLDL (Clopidogrel Dose dependent
aspirin less)
Clopidogrel

Inhibitors of Clotting Factor Synthesis

Warfarin Sodium Prevents carboxylation of Vitamin K - prevents Bleeding, allergy;Contra Oral; genetic variations
(coumarin) synthesis of II, VII, IX, and X in pregnancy, liver dx in susceptibility
Vitamin K Prevent synthesis of II, Also caused by diet, bowel dx, liver/bile dx
Antagonists VII, IX, X, proteins C, S (reduced synthesis); Pregnancy (inc. clot
factors)

Inhibitors of Clotting Factors

Heparin Anticoagulant - activates Also for asthma, growth hemorrhage, low Inhibits factors II, IX, X,
antithrombin III (& LPL) factor, antiviral platelets, osteoporosis and XII

Enoxaparin Low molecular weight

Heparin - inhibit factor Less capacity to bind Higher bioavailability,
Xa (less activation of platelet, plasma longer half-life
Dalteparin, antithrombin III) Anticoagulation, DVT proteins, or osteoblasts
Ardeparin prophylaxis, PE

Fondaparinux Indirect inhibitor of Xa NOT assoc w/ low Does not bind to platelet
synthesis platelets or osteoporosis factor 4

Protamine Sulfate Binds to Heparin- Reversing Can be used for Heparin

prevents its action anticoagulant state overdose

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Direct Thrombin Inhibitors

Bivalirudin, Derivative of hirudin - Originally from leeches

Lepirudin Prevents f.gen --> fibrin
Anticoagulation
Ximelagatran Synthetic thrombin Hemorrhage Oral
inhibitor (reduces fibrin)

Antithrombin III Inactivates thrombin (Iia) Hereditary AT-III Dizziness, chest pain,
and other factors deficiency nausea, chills

Fibrinolytic Agents

Streptokinase Bleeding, allergy, fever From Streptococcus

Tissue Plasminogen Decreased bleeding at aka Alteplase; prefers

Activator (t-PA) other sites (advantage) plasminogen on fibrin
Convert plasminogen Dissolution of formed
to active plasmin clots, evolving MI
 Convert plasminogen Dissolution of formed
to active plasmin clots, evolving MI
Urokinase

Anistreplase Complex of others

Drotrecogin Alpha Activated Protein C Sepsis Anti-inflammatory, anti-

thrombotic, profibrolytic

Antifibrinolytic Agents (Preserves clots)

Aminocaproic acid Lysine analog; inhibits

bnding plasmin w/ fibrin
Overdose of fibrinolytic
Tranexamic acid agents, stroke,
hyphema (blood in ant.
chamber of eye)
Aprotinin

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Stents with Anticoagulation Properties Inhibit proliferation of smooth muscle into lumen of
stent

Sirolimus Inhibit cell growth;

anti-inflammatory
Stents
Paclitaxel Inhibits phases of cell
cycle

Ionotropic Agents

Inhibits Na/K ATPase -> CHF, Atrial Nausea, vomiting, Increases automaticity
lowered intracellular K, flutter/fibrillation (slows diarrhea, visual and conduction in atrial
Digoxin increased intracell Ca, conduction through AV disturbances, various muscle; toxic levels can
increased release of node) arrythmias increase catecholamines
Ach
Milrinone increaes Ca influx CHF (IV) Tachyarrythmias (NOT Potent, but questionable
bradycardia) efficacy

Dobutamine Beta 1 agonist CHF (fixed, high grade Increases CO, and
(Enantiomers-some 'a') coronary occlusion) decreases VFP
Carvedilol, Beta blocking activity Reduce SNS effects in
Metoprolol CHF
Nesiritide (Brain Activates cGMP, CHF (IV) Is NOT arrhythmogenic
natriuretic peptide) Increases GFR

Anti-Arrythmic Drugs

Class 1A

Quinidine IV; Anti-muscarinic

Atrial, AV junction, Hypotension, syncope effects can -> tachyarr.
ventricular tachyarrys., (QT elongation) from
Block membrane Na including Wolff- Torsades de Pointes,
Procainamide channels, slow Phase 0; Parkinson-White cinchonism, SLE-like Sx NAPA metabolite can -->
ALSO block K channels, Torsades (like class 3)
prolongs AP and ERP
Disopyramide V.tach in those that Greater anti-muscarinic, Oral; aggravates
cannot tolerate first two -ionotropic, Torsades Myasthenia Gravis

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Class 1B

Lidocaine IV; ineffective in normal

V.tach in depolarized CNS effects, respond to polarized (Aflutter, Afib)
tissues (ischemic, dig. diazepam; Low
Block membrane Na toxicity), including WPW Torsades, hepatotoxic
Mexiletine channels, slow Phase 0 Oral form of lidocaine

Tocainide When other 1B's don't Agranulocytosis, aplastic Oral form of lidocaine;
work anemia, int pneumonitis requires CBC monitoring

Class 1C
Propafenone Long-term Na blocker, Proarrythmic effects,
slows all conduction Granulocytosis, SLE-like

Flecainide Long-term Na blocker, Life-threatening V.tach Decreased ionotropy, Oral; No anti-muscarinic

increased threshhold ONLY CHF, V.tach, Torsades Inc [] w/ Amiodarone

Moricizine Binds to Na channels in Proarrythmias, CHF, No anti-muscarinic

open state (lowrs Vmax) neurologic effects, shock

Class 2 (Beta blockers)

Propanolol Blocks B1 and B2; dec IV more effective

CO, -ionotropy, slow AV

Acebutolol More selective for B1 Conditions where Sinus bradycardia from

catecholamine excess is dec. slope of phase 4,
responsible for AV dissociation, rapid
Esmolol Short-acting B1 blocker generating autonomous removal can cause fatal
for after cardiac surgery ectopic rhythm disturbances,
(Pheocromocytomas, Bronchospasm,
exercise-induced hypotension
Labetalol V.tach), A.tach, PVC's
Both Beta and A1 block
Carvedilol Free radical scavenger

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Class 3

Bretylium K channel blocker, Life-threatening V.tach nausea/vomiting with Painful parotid

prolongs AP, ERP (old) rapid IV enlrgemnt, HTN in some

Amiodarone Na block, K block, Ca SV/V.tach, also WPW Pulmonary fibrosis, Active metabolite, NOT
block, a/b block (major DOC) corneal deposits, thyroid reverse rate dependent

Sotalol Beta blocker, increases SV/V.tach Bradycardia, Torsades Reverse rate dependent
AP & ERP in all tissues

Ibutilide Prolongs AP & ERP (Na Afib, Aflutter (better at Torsades Will not depress cardiac
channel agonist?) re-entry arrythmias) function; NOT RRD
Dofetilide Blocks rapid comp. of K Afib, Aflutter Never together with Better in Atria, RRD
delayed rectifier channel Verapamil

Azimilide K channel blocker, Afib LOW Torsades NOT RRD

prolongs AP, ERP

Class 4

Verapamil Decrease inward Ca Reentry SV.tach, Afib, Decreases ionotropy, Contra in WPW; blocks
current, slow AV Aflutter conversion Hypotension on cytosolic side
conduc, increase ERP,
slowed phase 4, HR Less -ionotropic
Diltiazem slowed AV node tachycardias effects blocks on exterior side

Unclassified Anti-Arrythmic Agents

Digoxin Reducing ventricular

Reduced AV conduction response Abnormal reentries (worse with hypokalemia),
to Afib/flutter treated with lidocaine

Adenosine K channel (A1) opener, Treating SV.tach, RAPID half-life (10sec); antagonizes
works in the nodes NOT Afib/Aflutter/Atach catecholamines, Diagnostic for SV.tach vs. V.tach

Atropine Anti-muscarinic: allows Bradycardias following

SNS to dominate MI's or Vasovagals

Isoproterenol Beta 1 and 2 agonst 2 or 3o heart block, Tachycardia, angina,

Stokes-Adams attacks tachyarrythmias

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Vasopressin Enhanced perfusion Vent. Fibrillation May be combined with

epinephrine

Magnesium Blockade of Ca, Na, K DOC for Torsades de Contra in complete heart
channels, ATPase pump Pointes block, renal failure

Potassium Hypokalemia, Torsades

if Mg not working
Drugs for Hyperlipidemia

Nicotinic acid (niacin) Inhibits mobilization of

free fatty acids (FFAs)
Inhibit VLDL synthesis,
induce LPL; inc. HDL
Gastric probs, Diabetes,
mylgia, rhabd., flushing 100% bioavailability

Lovastatin
Also: plaque stability, Lovastatin -
HMG CoA reductase anti-inflam., sepsis, Hepatitis, myalgia, prodrug/crosses BBB
Simvastatin inhibitors; prevents stroke, osteoporosis, rhabdomyolysis (esp. All increase hepatic
synthesis of cholesterol arthritis, DM, dementia, with niacin); slight LDL receptors;
MS, transplants, kidney increase in [warfarin] eliminated via CYP3A4
dz, cancer, blindness (big 1st pass)
Atorvastatin

Ezetimibe (Zetia) Inhibits cholesterol Often used with statin Gall stones? Inc. hepatic Eliminated via
absrp. (at brush border) enzymes; hedche, URIs glucoronidation

Cholestyramine
Bile acid sequestrants - Rash, fecal impaction, Increase hepatic LDL
Cholestipol prevent enterohepatic constipation receptors (need
recirculation (LDL now Can also bind drugs or cholesterol to make new
used to make more) vitamins --> deficiency bile acids)
Colesevelam

Gemfibrozil Inhibit VLDL synthesis, Allergy, RBC def.,

Activate peroxisome induce LPL, inc. HDL myalgia, rhabdo. (esp Fibrates
proliferators-activated Decrease with HMG-CoA inhib. & (fibric acid derivatives)
receptor alpha (PPARs) triglycerides niacin)
Clofibrate

Dietary Fiber Lowers cholesterol

Fish oil (Omacor) Decreased hepatic synthesis of fats and VLDL

Decreased platelet aggregation

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Drugs for Ishemic Heart Disease (Antianginal)

Nitroglycerin (GTN) Stimulate guanylate

cyclase --> Inc. cGMP
Relaxes smooth muscle
Antiplatelet; Abort MI
Headache, syncope,
flushing
Tolerance after 24 hrs to
patch method

Isosorbide dinitrate Vasodilator (arteries and Stable angina

veins) (also GTN)
Diltiazem Ca channel blocker Minimal reflex
sympathetic activation
HTN, angina, arrythmias
Verapamil Ca channel blocker Headache, flushing,
(L type) constipation, dizziness

Nifedipine Ca channel blocker Prinzmetal's angina, Reflex tachycardia

(dihydropyridine) HTN

Propranolol

Beta blockers
Timolol Increase diastolic time Improves subendo-
(inc. O2 supply) cardial flow, Dec HR,
Decrease Dec velocity of
Nadolol work of heart contraction
(dec. O2 demand)

Carvedilol

Aspirin Antiplatelet effects

Ticlopidine Antiplatelet effects See earlier

ADP antagonist

Abciximab Antiplatelet effects See earlier

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Hematopoietic Drugs

Iron Sulfate Cheapest, most widely

(Ferrous sulfate) used (20% iron)

Iron Deficiency Nausea, upper

Oral Iron supplement (Anemia) abdominal pain,
constipation, diarrhea
Ferric Gluconate Liquid form(Floradix):
(Floradix) better/faster absorption

Fe Fumarate 33% iron

Iron Deficiency Nausea, upper
Oral Iron supplement (Anemia) abdominal pain,
constipation, diarrhea
Fe Glycinate 27% iron

Fe Ammonium 16.5% iron

Citrate
Iron Protein Absorp. NOT affected by
Succinylate H2 antag, drugs, food

Molasses Source of iron Biproduct of sugar cane

processing
High risk of
Iron Dextran Anaphylaxis (need test
dose)
Hemodialysis w/ EPO, Injection site rxns,
Ferric Gluconate IV iron supplement Abnormal absorption, Diarrhea, nausea,
(Ferrlecit) intolerance to oral, oral Anaphylaxis
noncompliance Preferred due to less
adverse effects
Iron Sucrose
(Venofer)

Deferoxamine Iron chelator Iron toxicity (overdose)

Cyanocobalamin IM B12 injection B12 deficiency (inc. Cold abscesses Very painful
methylmalonic acid)

Methyl Cobalamin Sublingual B12 NO B12 toxicity (for all

methods)

Folic Acid Oral, IV, IM, SC Deficiency/Prophylaxis To prevent neural tube

in pregnancy defects
Procrit, Epogen Iron supplement likely
(epoetin alpha) Chronic renal failure, CV events, HTN, (all forms)
EPO analogs- induce AZT pts (suppress BM), seizures, thrombosis
RBC maturation Chemotherapy pts, (esp. renal failure); also
Aranesp Chronic inflammation Abuse potential! Longer T1/2, lower
(darbepoetin alpha) binding affinity

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Sargramostim Recombinant GM-CFS- Chemo in AML patients Bone pain, pulmonary Pulmonary capillary leak
(Leukine) > granulocyte/macros (>55yo), BM transplant edema, heart failure --> syndrome, fever, mlaise
Filgrastim
(Neupogen) Recombinant G-CFS -> Chemo in AML patients Bone pain, splenic Better tolerated than
neutrophils/granulocytes (>55yo), BM transplant,
to prevent neutropenia neutrophil ARDS
rupture, from GM-CSF, Neulasta
prolonged action (slow
PEG-Filgrastim (NO macrophages) (infections) infiltrate lung renal clearance)
(Neulasta)

Hematide Stimulates EPO

In clinical trials
CERA EPO receptor agonist
(long lasting)

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Prostaglandins Inc. cAMP --> Dec Ca2+ Peripheral Vascular Dz Virtually all tissues, act
--> vasodilation (PGE and PGI2) locally, rapidly metaboliz

Alprostadil PGE1 Patent Ductus arteriosis

Erectile Dysfxn

Misoprostol PGE1 analog NSAID-induced ulcers Stimulates contraction

--> preterm labor Can cause abortion

Dinoprostone PGE2 Abortion, Induced labor Abortion in combo w/

Misoprostol and MTX

Epoprostenol PGI2 (Prostacyclin) Pulmonary HTN Inhibits Platelet agg Mainly in endothelial
(emergency) cells

Prostaglandin F2a PGF2a

Carboprost PGF2a analog Off US market

Latanoprost PGF2 analog Glaucoma (topical) -

increases humor outflow
TXA2 (Inc. IP3 --> Inc Mainly in platelets - in
Thromboxane Promotes Platelet agg response to injury
Ca2+ --> vasoconstrict)

Summary All induce labor

PGE2 and PGI2 Vasodilation, Bronchodilation, DEC platelet agg, INC renal blood flow, GI (dec acid, inc HCO3&mucus)

TXA2 and PGF2a Vasoconstriction, Bronchoconstriction, INC platelet agg (TXA2)

CNS neurotransmitter
Constricts Bronchi (H1) (H1 and H2)
Histamine Constricts Gut (H1)
Inc Gastric Acid (H2)
Vascular dilation (H1,2) Nerve endings (Pain, BP drop (H1 rapid, H2
itch) - (H1) slow effect)
 Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

1st Gen. Antihistamines

Diphenhydramine
(Benadryl) Minor Allergic reactions
(edema, rash, itch), CNS effects: Sedation, Contraindicated in
Dimenhydrinate Block H1 Allergic rhinitis Antitussive, Dec motion asthma due to drying
(Dramamine) (hay-fever, hives), sickness (antiAch?), effect on lungs
Motion sickness, dryness
Chlorpheniramine Sedative OTC
(Chlor-Trimeton)

2nd Gen. Antihistamines

Fexofenadine
(Allegra)
Little/NO sedation Do NOT cross BBB
Minor Allergic reactions (NO CNS)
Loratadine (Claritin) Block H1 (edema, rash, itch), NOT antiAch
Allergic rhinitis NO motion sickness
help
Cetirizine (Zyrtec)

Terfenadine Converted to Allegra via

CYP 3A4 --> Block H1 CYP inhibitors Off US market -
(ketoconazole, Torsades de pointes!!
erythromycin) --> toxicity (esp w/ hepatic dz)
Astemizole Block H1

H2 Receptor Antagonists

Cimetidine
(Tagamet)

Ranitidine (Zantac)
Block H2 - Decrease
gastric acid secretion GERD, Ulcers
(volume and acidity)
Famotidine (Pepcid)

Nizatidine (Axid)
 Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Drugs for Migraines 5-HT1 agonists

5-HT2 antagonists
TREAT current migraine
PREVENT future ones
Treatment aimed at
vasoconstriction

Ergot alkaloids Partial agonist (alpha Migraines, cluster Ergotamine, caffeine,

and 5-HT) - vasoconstric
5-HT2 antagonist
Methysergide
(prevent vasoconstrctn)
5-HT1D agonist (reverse
Sumatriptan
vasodilation)
Propanolol (and Beta blocker - may have
other B blockers) action at 5HT receptors
Diltiazam, nifedip- Ca channel blockers -
ine, verapamil may involve 5HT receps migraines, clusters
headaches dihydroergotamine
All prophylactics require
Prophylaxis weeks to be effective
Terminate acute Also (naratriptan,
migraine No dependency risk rizatriptan, zolmitriptan)
Prophylaxis Dec platelet agg
Prophylaxis of Migraine-like headaches Dec frequency, little
effect on severity

Lithium carbonate Prophylaxis of chronic

cluster headaches
NSAIDS + barbitu- Abort a migraine
rate and caffeine

Classification of NSAIDS
 Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Cleared by conjugation - Low dose (1st order)

Fever, headache,
Inhibit COX - ASA irrev. myalgia, neuralgia,
Salicylates (Aspirin, All others reversibly... dysmenorrhea,
etc) Blocks osteoarth., rheumatoid, Salicylism: tinnitus, hache, N/V, dizzy, vision
TXA2 required for prophylaxis for heart,
platelet aggregation Gout (high dose)
High dose (0 order); High dose -> uncouples
oxidative phosphorylation -> Hyperventilation
and respiratory alkalosis; dose can -> acidosis;
Gastric bleeding (->Fe def?), GI probs, Ulcers?,
High frequency hearing loss (reversible),
Lipooxygenase activation may ->
Hypersensitivity (asthma/nasal polyps)
Also Reye's syndrome (w/ viral
infxn)

Methyl salicylate Topical use only

(Ben-Gay)

Salicylic acid Keratolytic Acne, seborrhea, warts

Little/NO anti- NOT an NSAID

inflammatory, Low GI, Peroxides->Inactive
No effect bleeding/resp Can affect ASA
Acetominophen Weak inhibitor of COX Analgesic, Antipyretic Not uricosuric binding Greater effect
Hepatic necrosis in CNS? Free radical
(esp. EtOH, fasting) metabolite
Renal tubular necrosis

Celecoxib Contains Sulfa

(Celebrex) Selective COX-2
Inhibitors (reversible) Osteoarthritis, Acute Gastric bleeding? Heart
(Little effect on COX1) pain, Menstrual pain attacks, Stroke
Rofecoxib (Vioxx)

Ibuprofen COX inhibitor (NSAID) Same as ASA (better for GI (N/V), CNS - dizzy, Cross sensitive ASA
dysmenorrhea) headache, etc. Naproxen - long acting
 Intractable fever Sulindac - prodrug with
Indomethacin COX inhibitor (Most (Hodgkins), ankylosing Frontal headache, GI less toxicity
potent one) spond., OA, RA, GoutA ulcers, blood loss Contraindicated: Ulcers
close patent ductus Pregnancy, Psychiatric

Ketorolac COX inhibitor Short-term analgesic Hepatic, renal toxicity Only IM NSAID
(compare opioids, etc) No evidence of abuse

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Diflunisal NO antipyretic Poor entry to CNS

Diclofenac Accumulates in synovial

fluid - rapid onset

Etodolac Similar to indomethacin

Nabumetone Prodrug, ketone ->

acetic acid derivative
COX inhibitors (NSAIDs)
Meclofenamate May also block PG
receptors
Piroxicam
(and other "- Long T1/2
cams")
Tolmetin May be better tolerated
than ASA

Phenylbutazone Avoid! Many severe

Slow-Acting Antirheumatic Drugs (SAARDs) - Disease-Modifying Antirheumatic Drugs (DMARDs)First line: NSAIDs

Hydroxychloroquine Hemlytic anemia(G6PD) Least toxic of all

(Plaquenil) Retinal damage-elderly SAARDs
Mild RA
Sulfasalazine HA (G6PD), Naus, rash
(Azulfidine) Leukopenia, hepatitis

Methotrexate (MTX) Moderate RA Hep.enzymes, Dec BM High response rate; Oral

(Often DOC) teratogenic, stomatitis weekly dose, FA supple
Leflunomide (Arava) Infrequent (usually in Diarrhea, alopecia, hep. Less expensive, higher
combo with MTX) enzymes, teratogenic toxicities

Gold (injectable) Stomatitis, rash, Weekly CBC and UA

proteinuria
Azathioprine Metabolized to 6- Immunosuppresive
(Imuran) mercaptopurine

Anakinra IL-1 antagonist If failure w/ TNF

Inhibits inflam effects inhibitors

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Etanercept Soluble TNF receptor -

antagonizes TNF

Infiximab Risk of serious infections Require TB screening

and lymphoma before use
Anti-TNF Monoclonal
AB
Adalimumab

Anti-Gout Drugs Tx: Reduce inflam/production of uric acid; increase excretion

NSAIDs (NOT ASA) Decrease pain/inflammation, Dec phagocytosis of

urate crystals -> more excreted
Initial Tx, or sub. for
Colchicine
Indomethacin most
common

Colchicine Binds to tubulin, inhibits Acute Gout (1st line) - Diarrhea, N/V Reduces leukocyte
polymerization 12-24hrs till effect migration/inflammation
Inhibits Xanthine Oxids Chronic Gout (often in Prolongs T1/2 of 6-
Allopurinol Reduces uric acid syn. combo to start) Uncommon
mercaptopurine

Rasburicase Recombinant urate Expensive

oxidase - breaks urate

Probenecid Contains Sulfa

Weak organic acids - Compete w/UA for
increase excretion of UA transport (reabsorption)
Sulfinpyrazone
Drugs for Asthma and other Inflammatory Pulmonary Diseases

Beclomethasone
Adrenocorticosteroids - Systemic: Adrenal sup,
Decreases inflam. and Growth retard, Osteo, Side effects much less
Flunisolide secretions/mucus/ Cataracts, Blood with aerosol route and
cytokines; increases B changes, Weight gain, alternate-day method
receptors in lungs HTN
Triamcinolone

Ipratropium Br & Anticholinergic - blocks

Atropine M3 receptors

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Theophylline GI upset, anxiety,

Methylxanthines - PDE Reduce LT actions, arrhythmias, seizures Anti-inflammatory effects
action, Ca action, Cate- Dilates, Inc work able, via effects on
Aminophylline cholamines, endogenus CNS stimulant, diuretic eosinophils
Caffeine

Epinephrine Most cardiac effects

Albuterol Least cardiac effects, (more B2 selective)

Tremor

Terbutaline
B-adrenergic agonists -
1) Relax bronchial SM Asthma, Bronchitis,
Salmeterol 2) Stimulate Emphysema (more
mucocilia 3) Dec. effective in COPD)
SM hypertrophy 4)
Inhibit inflam. cells More cardiac effects
Isoproterenol than albuterol

Fluticasone

Formoterol

Cromolyn Sodium Inhibits cellular actvaton Mast cell stabilizer, Inhibits eosinophil
(Cl channels) inhibits cough infiltration

Water Most effective Few (sposed to liquify Inhaled steam/vapor

expectorant bronchial secretions)

Expectorants
Potassium iodide Expectorants Also Ipecac (subemetic
dose)
Mucokinetic agent
Guaifenisin

Acetylcysteine Splits disulfide bonds Bronchitis, COPD,

-> less viscosity Acetominophen OD

Dornase Recomb. DNAase -> Cystic fibrosis, Chronic Cough, wheeze, Aerosol
Cleaves mucus bronchitis hemoptysis, pharyng

Amrinone
PDE3 inhibitors Bronchodilation -
Asthma
Enoximone

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Ipopamine

Milrinone
Phosphodiesterase Bronchodilation - Nausea and vomiting
Inhibitors --> Asthma may limit use of PDE4
Bronchodilation inhibition
Vesnarinone

Pimobendan

Verapamil
Ca channel blockers Relax bronchial SM,
"stabilize" membranes
Nifedipine

Zarfirlukast
Leukotriene receptor Food decreases
Antagonist (nonspecific) Increase theophylline bioavailability
Montelukast and warfarin
Met. by CYP2C9,3A4
Zileuton 5-lipooxygenase Headache, hep. toxic
inhibitor Dyspepsia

Omalizumab Anti-IgE monoAb Headache, viral inf., SC admin only

thrombocyto, allergies
Drugs for Gastrointestinal Disorders

Peptic-acid Disorders

Omeprazole PPI Prodrug - oxidizes Zollinger-Ellison Inhibits P450; rash, hep *Acid suppression
(Prilosec) SH groups in pump syndrome DOC*, GERD enzymes, constipation (irreversible), long effect
Lansoprazole GERD
(Prevacid)

Rabeprazole Proton-pump inhibitors

(PPIs)
Esomeprazole &
Pantoprazole

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

NaHCO3 Alkalosis when Last much longer when

prolonged, UTI, gas given with food
Antacids - neutralize No alkalosis, rebound
CaCO3 (Tums) HCl (Do NOT inhibit acid hypersecretion Non-systemic
production)
Mg(OH)2, Al(OH)3 Diarrhea, renal excretion (Mg)Most potent (Al)Low
Milk Alkali syndrome phos, Alzehimer?

Simethicone De-foaming action - Antiflatulent, GERD

coalesces gas bubbles
Cimetidine Headache, dizziness, GI, low sperm,
(Tagamet) gynecomstia, menstrual, halluc, agitation, apnea,
renal failure
Ranitidine (Zantac) Lacks the hormonal 5x more potent than
H2-receptor antagonists adverse effects Cimetidine
(usually combo with Prevent ulcer
Famotidine (Pepcid antibiotics for H.pylori) Less hormonal and drug <160x more potent than
AC) interaction effects Cimetidine

Nizatidine Does not inhibit P450 Similar to Ranitidine,

higher bioavailability

Propantheline Similar to conventional Contra: glaucoma,

systemic effects obstructive uropathy,
(inc pulse, dryness, arrhythmias, myasthenia
M1-muscarinic receptor blurry vision, etc) gravis
antagonists
(anticholinergic)
 Similar to conventional Contra: glaucoma,
systemic effects obstructive uropathy,
(inc pulse, dryness, arrhythmias, myasthenia
Methantheline M1-muscarinic receptor blurry vision, etc) gravis
antagonists
Pirenzepine (anticholinergic) Contra: Above except
More selective to glaucoma
stomach - less adverse
(Pirenzepine - no CNS) More potent -
Telenzepine investigational in US
PGE1 analog - Mucosal protection for Diarrhea, N/V, Uses EP3 recps, gastrin
Misoprostol Decreases cAMP chronic NSAIDs uterotonic -> abortion mucus/HCO3 secretion

Sucralfate Small amount of Al Mucosal Protection Rare; may impair NOT in combo with
absorbd: paste on ulcer absorption of others antacids/indomethacin
Bismuth Reacts w/ HCl -> Ulcer, mucosal Black stool/tongue (Pepto-Bismol)
Subsalicylate salicylate; H.pyloricidal protection

Proglumide Gastrin receptor blocker

Sulpiride Antidopamine - inhibits NOT approved in US

gastrin release

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Laxatives (and Cathartics) Persistent constipation, Cathartic colon syndrome, Addiction, Hypok+,
CV dz, hernia, parasites Malabsorption, Liver abnormalities (DSS)

Castor oil PGE2->cAMP also Bad taste Act: ricinoleic acid

inhibit Na/K ATPase
Emodin alkaloids Inhibit Na/K ATPase -> Danthron-hepatic/intest Must be activated by
(cascra, aloe, sena) water accum in lumen tumors; Others-colic bacteria (delay action)
Irritant/Stimulant
laxative
Phenolphthalein Inhibit Na/K ATPase, Carcinogen - Removed Must be absorbed
Increase cAMP and from market glucoronidated
PGE Increase intestinal
injury Increase K
Bisacodyl permeable Oral and rectal
Fiber-Hphilic Cellulose fibers take up Few, requires LOTS of Also for acute diarrhea
colloids (bran, water -> swell water (soak up water)
psyllium, etc)
Polyethylene glycol Isosmotic lavage Bulk forming laxatives Electrolyte solution
(PEG - GoLytely)
Saline (and other Osmotic For evacuation before
salts) procedures
Docusate Inhibit Na/K ATPase Minimal laxative effect
Increase cAMP
Glycerin Stool softeners No salts present
suppositories
Mineral oil Fat Vitamin def. Leaks past anal
(Liquid petrolatum) sphincter

Antidiarrheals

Diphenoxylate Analog of meperidine

Opioids - effects on
Loperamide smooth muscle and Minor More potent
(Imodium) mucosa --> inc.
electrolyte transport Diarrhea
. Potent metabolite of
Difenoxin Role of nerve plexi CNS effect Diphenoxylate
and mu receptors
Paregoric Camphorated tincture of
opium

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Bismuth salts Absorbs toxins of E.coli, Black tongue/stools, Traveler's diarrhea

Decreases PG, cAMP Impaction

Kaolin Diarrhea
Thickeners and water Kaopectate
binders
Pectin

Emetics and Antiemetics and GERD

Ipecac Emetic Must enter CNS (delay)

Active ing: emetine
Act on CTZ in 4th vent.
Apomorphine Emetic, Parkinson's More toxic than ipecac Morphine deriv. w/ no
(DA analog) analgesic; SC=faster
Scopolamine Anticholinergic Dry mouth, blur vision, Dermal patch behind ear
drowsiness
Dimenhydrinate
(Dramamine)
Antiemetics
H1-receptor antagonists Drowsiness-less so with Used for motion
Meclizine Central anticholinergic? meclizine sickness, vertigo,
nausea of pregnancy
Cyclizine

Dronabinol (THC) N/V, Anorexia in AIDS Sedation, psychoactive For cancer-

patients chemotherapy

Ondansetron
5-HT3 antagonists Pre-Tx for Constipation, diarrhea,
Work in CTZ Chemotherapy HTN, Hep. enzymes
Nausea/vomiting
Granisetron

Chlorpromazine Inhibit DA, Ach, His, and Post-op and post-rad. Works in emetic center
(Phenothiazines) alpha receptors Nausea/vomiting (oral/IV/rectal)

Metoclopramide Dopamine receptor D2 GERD Diarrhea Increases tone of

antagonist -> inc. tone esophageal sphincter

Cisapride 5-HT4 agonist Nocturnal heartburn Selective availability

(Indirect Ach agonist) (GERD), constipation NO effect on DA system

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Inflammatory Bowel Disease

Mesalamine (5-ASA) Inhibit PG and Leukot.

Formation Upper GI irritation,
watery diarrhea,
nephrotoxicity,
Olsalazine Two molecules of 5-ASA pancreatitis 5-aminosalicylic
linked --> split preparations (5-ASA)
Split into 5-ASA and Inflammatory bowel dz *BM suppression, liver
Sulfasalazine sulfapyridine* (Ulcerative colitis, failure, male sterility
Chron's)
Hydrocortisone
Steroids - reduce Same as systemic when
inflammation chronic
Prednisone
Infliximab IgG MonoAb for TNFa Chron's infusion reactions,
infections

Anticholelithics

Ursodiol Prevents absorption of Less diarrhea Also promotes

dietary/biliary cholest. mobilization from stone
Inhibits 3-OH-3CH3glut Dissolution of gall Also breaks up stones,
Chenodiol stones Diarrhea NO effect once
CoA reductase calcified
Monoctanoin Fatigue, Ab pain, N/V, Infused into common
diarrhea, pruritus bile duct

Irritable Bowel Syndrome (IBS)

Tegaserod 5-HT4 agonist - Women w/ IBS w/ Heart attacks, stroke, Removed from market
stimulates motility Constipation (shorterm) headache, diarrhea

Alosetron 5-HT3 antagonist - Women w/ IBS w/ Serious GI (fatal) Met. by P450

modulates enterics Diarrhea

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Toxicology

Oxygen

D50W (sugar)
Initial Tx for
unresponsive patient
Thiamin

Naloxone
Fomepizole (4- Methanol poisoning NO CNS
methylpyrazole) effects/depression
N-acetylcysteine Acetaminophen OD
(NAC)

Desferoxamine Iron OD

Dimercaperol Arsenic poisoning

(NOT arsine)
Polyethylene glycol Lithium, Cadmium, Fe Whole bowel lavage
(PEG - GoLytely) poisoning

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Complimentary and Alternative Medicine

Garlic High lipids, HTN, ather- Induces CYP3A4, anti- Can cause bleeding w/
osclerosis, Cancer thrombotic, antiplatelet surgery

Echinacea Colds, Flu Controversial

effectiveness
Glucosamine Osteoarthritis, TMJ Shellfish allergy Does NOT affect insulin
(sulfate) arthritis levels
(Panax) Ginseng Fatigue, "Adaptogen" Insomnia, Nervousness

Lutein Carotenoid Age-related macular

degeneration (before)

Ginkgo Alzheimer Dz, Memory Interactions (CYP?), Some positive evidence

enhancer, Claudication Seizures, Delayed onset for all 3 uses

Soy Estrogenic (low) & Menopausal Sx, Breast Lymphocytopenia w/ Mech depends on
Antiestrogenic (high) Cancer certain derivative endogenous levels

Kava Anxiety (short term) Hepatotoxicity, Sedation CYP2D6 required to

w/ other CNS depresnts metabolize

Valerian GABA agonist Insomnia, Anxiety Additive sedation Prolonged anesthesia w/

surgery

Saw Palmetto BPH (minor) No effect on PSA, Similar to finasteride

No impotence effectiveness

St. John's Wort Depression (mild to 5-HT Syn. w/ SSRI's, Similar to TCA
moderate) Induces CYP effectiveness

Chondroitin Osteorthritis Role in Prostate cz? Similar to NSAID

effectiveness

Black Cohosh Menopausal Sx Hepatitis (rare)

Coenzyme Q10

Bitter Orange Sympathomimetic (like Weight loss ("Ephedra- Hemorrhagic stroke, Contains tyramine, is
phenylephrine, norepi) free") inhibits CYP3A4 similar to Ephedra