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Justin Cohen's Sweet P-Sheet

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Direct Cholinergic Agonists Note: Do not use if


Bowel obstruction,
Muscarine Muscarinic Asthma, Peritonitis No CNS action

Nicotine Nicotinic

Pilocarpine Pred. Muscarinic Glaucoma, Xerostomia

Stimulate Bladder, GI,


Bethanechol Pred. Muscarinic 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
Myasthenia Gravis,
Neostigmine
Urinary retention, etc
Excess can cause
Physostigmine Anticholinesterase Glaucoma, CNS seizures Depolarizing
Neuromuscular Blockade
Myasthenia Gravis,
Pyridostigmine
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
Organophosphate cov-
Echothiophate Glaucoma Duration is >1 week
alent bond w/ Esterase
Mammals can inactivate,
Malathion Pediculosis (lice)
Insects can't (pesticide)
Nerve Gas (Soman, Phosphorylated Esterase Pralidoxime (2-PAM) can
None
Tabun, VX) that cannot regenerate help if early (No CNS)

Acetylcholine Augmenters

Sildenafil (Viagra) Differences due to


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

Cholinergic Antagonists (Antimuscarinics)

Atropine Eye dilation Aggravates Glaucoma

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


Scopolamine
mydriasis, cycloplegia restlessness, delerium Atropine
Muscarinic competitor
Homatropine Short duration, synthetic
blocks M1, M2, and M3
Muscarinic competitor
blocks M1, M2, and M3

Propantheline Synthetic

Inhalation Less due to minimal lung Local action taken as


Ipratropium
Bronchodialator absorption mist, Synthetic

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Pirenzipine Blocks M1 in ganglia

Blocks M3 in parietal Ulcers (oldfashioned),


Dicyclomine
cells relaxing smooth muscle
Blocks M2 and M3 in more selective to
Tolterodine (Detrol) Hyperactive bladder
Bladder bladder

Cholinergic Antagonists (Antinicotinics-Ganglionic blockers)

Hexamethonium Emergency HTN crisis


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

Cholinergic Antagonists (Antinicotinics-Neuromuscular Junction blockers)

Tubocurarine Given IV or IM

Pancuronium Some association with


Non-depolarizing
blockade of Nnmj receptor Muscle relaxation before Histamine release due to
Mivacurium and during surgery, large size
Competes with Ach at (bronchospasm and
ECT, Tetanus
receptor edema)
convulsions, orthopedic
procedures
Non-depolarizing Some association with
blockade of Nnmj receptor Muscle relaxation before Histamine release due to
and during surgery, large size
Competes with Ach at (bronchospasm and
ECT, Tetanus
receptor edema) Seizures due to
Atracurium convulsions, orthopedic
procedures metabolites in CNS
Excreted by liver (used
Vecuronium
in Pts with renal probs)
Depolarizing blockade of Contract then paralyzed
Succinylcholine Nnmj receptor Malignant hyperthermia
(Pseudocholinesterase)

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Other "Muscle Relaxers"

Unknown; Decreases Ca
Dantrolene Malignant hyperthermia Hepatotoxicity
release from SR
Blocks Ach vesicle Prevent sweating,
Botulinum toxin
release (for months) cosmetic
Black Widow Spider Massive release of Ach
Venom from vesicles

Direct Adrenergic Agonists (Sympathomimetics)

Low dose: B (dilation) Asthma, anaphylactic CNS effects (tremors,


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

Dobutamine Beta 1 (some Alpha) Increase CO in CHF

topical, eye, nasal


Phenylephrine Alpha 1 >> Alpha 2 reflex bradycardia
decongestant
Paroxysmal supravent.
Methoxamine Alpha 1 Does not stimulate heart
tachycardia
Similar to Albuterol,
Metaproterenol Beta 2 Bronchodilator
Ritodrine, Terbutaline
Isoproterenol Beta 1 and Beta 2

Control of BZ and opiate Inhibits sympathetic


Clonidine Alpha 2 (in CNS)
withdrawl vasomotor centers

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Indirect Adrenergic Agonists

Beta 1 and alpha


Amphetamine
mediates Norepi release
Metabolized by MAO
Tyramine causes release of Norepi
(careful with inhibitors)
Beta 1 and alpha Local anesthetic activity blocks reuptake of Peripheral and CNS
Cocaine
blocks Reuptake 1 with analogs Dopamine and Norepi effects
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
Pseudoephedrine Norepi

Direct: a
Metaraminol Hypotensive states No CNS-too polar
Indirect: rel. of Norepi

Alpha-Adrenergic Antagonists

Decreases TPR and blood


Phenoxybenzamine Pheochromocytoma orthostatic hypotension
Non-selective alpha pressure
blocker
Non-selective alpha
blocker reflex tachycardia can
Phentolamine
worsen heart condition

Doxazosin

Tamsulosin nasal congestion, Decreases TPR and blood


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

Prazosin

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Beta-Adrenergic Antagonists

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

Timolol Topical for glaucoma

HTN with impaired Will not block B2 (no


Atenolol
pulmonary function added lung problems)
Selective Beta 1 blocker
Metoprolol

Agents with Intrinsic Sympathomimetic Activity

Not pure B antagonists HTN in Pts who cannot


Pindolol, Acebutolol
Partial agonists tolerate increased TPR

Beta and Alpha 1 Antagonists


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

Other Agents with Adrenergic Agonistic Activity

inhibits storage of Depletes Norepi with


Reserpine
Norepi in vesicles decrease in sympathetic
blocks release of stored
Guanethidine
Norepi

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Local Anesthetics

Short-acting, Ester
Procaine
(PABA metabolites)
Anesthetic… blocks C- CV, CNS depression,
Lidocaine Blockade of Na+ channel Intermediate-acting
fibers, then Adelta- Antiarrhythmic
in membrane… prevents
fibers, then Aalpha
Bupivacaine depolarization Long-acting
motor fibers

Benzocaine Topical only

Other Agents with Na+ Action

Tetrodotoxin Puffer fish poison


Binds near Na channel
Blocks opening
Saxitoxin Red tide

Binds within channel


Scorpion Venom
Prevents inactivation
General Anesthetics

Surgery, Recreational Minor CV, resp and SM Gas, rapid onset and
Nitrous Oxide
(Whip-its) effects, CNS toxicity recovery (low lipophilic)
Blunts resp, CV, uterus, No analgesic effect,
Halothane
Malignant hyperthermia reactve metabltes->Hep
Surgery
Ion channels, signal Greater Resp. Used a lot, not good with
Isoflurane
transduction depression, bad odor longer procedures
Analgesics, not much Most potent of gas
Methoxyflurane Labor and delivery
uteran; Nephrotoxicity agents

Sevoflurane Surgery little CV or organ toxicity limited metabolism

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

CNS Depression
Thiopental GABA receptors Resp and CV toxicity Induction Agent
(anesthetic)
Midazolam, Valium Potentiation of GABA Conscious sedation with Countered with
(Benzodiazepines) (inhibitory effects) amnesia Flumazenil
Induction (replaced
Propofol Decreased TPR
Thiopental)
Vomiting, Nausea, pain
Ethomidate Hypnotic No analgesic effects
on injection
Replaced morphine and
Fentanyl (Opiods) Analgesia w/ amnesia Less CV effects
meperidine
Catatonia without CV or Similar to PCP: weird
Ketamine NMDA antagonist Dissociative anesthetic
Resp depression dreams/visions, inc ICP

Drugs for Parkinson's (loss of DA action)

Coenzyme Q10 Can slow progression

Large first-pass, to CNS


Levodopa (L-Dopa) Converted to Dopamine Parkinson's Disease Similar to DA (but less)
by ACTIVE transport
Does NOT cross BBB
Blocks AAAD in Periph. Lessens peripherals,
Carbidopa (prevents --> DA in
More L-Dopa in CNS may increase CNS ones
Per.)
Preventing DA Type B more specific to
Selegiline (deprenyl) Inhibits MAO type B Adrenergic stimulation
metabolism DA at small doses

Entacapone Inhibits COMT Prevent DA metabolism NO hepatotoxicity


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

Bromocriptine Still active at later For all DAergic drugs:


stages when DA Per - arrythmias (B1),
Pergolide neurons completely lost hypotension
CNS -N/V(emetic center)
Dopaminergic agonists Cross BBB
dyskinesias, agitation,
Pramipexole hallucinations (DA
receptors in other parts
Ropinirole of brain)

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Other Drugs for Parkinson's

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

Synthesis, release, Antiviral, seemingly Livedo reticularis (bluish


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

Amphetamine Blocks reuptake of DA

Parkinson's Drug Interactions

Can worsen PD Can lower effectiveness


Antipsychotic drugs DA-receptor antagonists
symptoms of PD drugs
Co-factor for L-Dopa Supplementation can
Pyridoxine (Vit. B6)
metabolism decrease [L-Dopa]
Increases levels of NE, MAO inhibitors can
Tyramine HTN crisis --> Death
can also act directly prevent breakdown

Drugs for Hyperkinetic Disorders (loss of GABA action)

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

Does NOT cause Tardive


Clozapine Atypical antipsychotic
Dyskinesia
Nonselective Beta
Propranolol Tremors
Blocker

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Drugs for Psychiatric Disorders (Antipsychotics)

D2 blockers Block DA type 2 Positive symptoms Usually safe, unless Blockade of DA's in other
receptors (delusions, craziness) combined (EtOH), parts of brain, or other
5HT2 blockers Block 5-HT type 2 Negative symptoms increased Prolactin with receptors (Ach,His) can
receptors (anergy, depression) DA blockade, TD, lead to side effects
Antipsychotic malignant
Phenothiazines syndrome

Also antiemetic,
Chlorpromazine First antipsychotic drug
antihiccup
Arrhythmias w/ overdose High sedation, alpha-
Thioridazine
Pigmentary retinopathy blockade, Low EPS
Depot preparation for
Fluphenazine
compliance probs

Classical antipsychotics -
Reduce dopamine action
Perphenazine

Classical antipsychotics -
Prochlorperazine
Reduce dopamine action

Thioxanthines

Thiothixene

Butyrophenones

Most widely used of Low sedation, alpha- Depot preparation for


Haloperidol
classical antipsychotics blockade, High EPS compliance probs

Heterocyclic (newer agents)

Requires WBC Agranulocytosis, Increased antimuscarinic


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

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Fatigue, hand tremor Behaves similarly to Na+


Bi-Polar disorder
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

Possible birth defects, Also used for pain control, diabetic neuropathies,
Antiepileptic Drugs
OC interactions and withdrawl symptoms control
Like Phenytoin; + DOC Drowsiness, vertigo,
Carbamazepine NOT used for Absence
for Trigeminal Neuralgia ataxia
Block Na channels in
+ (petit mal) seizures;
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
More hydrophilic IM/IV;
Fosphenytoin
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)
GM, Psychomotor, and Least toxic; --> Children
Phenobarbital Sedation or hyperactivity
Focal; also (EtOH w/x) to avoid gum growth
Metabolized to Allows for greater activity with less blood levels of
Primidone Myoclonic in children
Phenobarbitol and PEMA Phenobarbital, therefore less sedation
Blocks T-type Ca2+ Absence (petit mal) Extended depression
Ethosuximide (1o) Contra in tonic-clonics
channels ONLY -- usually children (GI, drowsiness, lazy)
Useful in all, esp. Drowsiness, ataxia, Potential to exacerbate
Clonazepam Stimulates GABA
myoclonic and akinetic aggressiveness seizures; yes Tolerance

Diazepam Status epilepticus Medical emergency

Therapeutic Adjuncts (some can be used alone)

Clorazepate Converted to Diazepam Prodrug

Blocks NMDA? Aplastic anemia, GI, and 0-order, increases


Felbamate Partial sz in Adults
Potentiates GABA? CNS [valproate,phenytoin]
Partial sz; Pain control -
Gabapentine Increase GABA release?
(more common use)

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Partials, some GM, Cerebellar dys, Possibly leading to


Lamotrigine Inactivates Na+ channels
atonic, and absence drowsiness, and rash Stevens-Johnson syn.
Blocks Na+ channels, Partial sz (approved for Also inhibits glutamate
Topiramate Ataxia, drowsiness
augments GABA monothrpy), migraines at certain receptors
Irreversible inhibitor of Complex Partial sz Psychotic rxns,
Vigabatrin Not available in USA
GABA transaminase (Psychomotor) hyperactivity

Levetiracetam Partial sz

Zonisamide Partial sz Newer agents


Newer agents

Tiagabine Blocks GABA reuptake Partial sz

Another option for


Lorazepam
status epilepticus

Presynapse: close Ca2+ Effects of receptors (Mu,


Opioid Agonists
Postsynapse: open K+ Delta, Kappa)

Histamine release due to


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

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


Meperidine
Avoid chronic use from metabolite NO miosis (abuse!)
Withdrawl from heroin Less euphoria, slow Slower onset, longer
Methadone
or morphine withdrawl duration of action
Anesthesia (sedative, 80x better analgesic Transdermal form -
Fentanyl
analgesic) potency than morphine slower onset, long DOA
Metabolized in liver to Cough, Pain relief (w/ Some people lack
Codeine Decreased dependence
morphine by CYP2D6 NSAIDs) CYP2D6 (no pain relief)
Oxycodone,
Mild-moderate agonists Pain control
Hydrocodone

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Cardiotoxic, Pulmonary No benefit over other


Propoxyphene Derivative of Methadone Weak analgesic
edema drugs; use declining
Partial agonist (Mu, Withdrawl sx when given Talwin-NX to prevent IV
Pentazocine Analgesia (kappa)
delta, sigma) with morphine abuse

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

Sedative-Hypnotic and Anxiolytic Drugs

Tolerance --> Smaller


Barbiturates
Therapeutic index

Phenobarbital Enhances duration


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

Miscellaneous

Partial agonist at 5-HT1a Does not interact with 1-4 weeks to start
Buspirone Anxiety only
receptors EtOH, motor skills working
Non-selective beta Chronic anxiety, panic Contra: Diabetics,
Propanolol
blocker attacks asthmatics
Zolpidem (Ambien), Selective for BZ1 Less tolerance,
Hypnotic similar to BZ's
Zaleplon receptor (sleep) dependency, amnesia
Rapid onset, short
Chloral hydrate Low TI Unpleasant taset/smell
duration

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

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


Benzodiazepines
memory/motor function few outside of CNS anesthesia or death
All of these can cross
Alprazolam
placenta --> probs.
All these only toxic when
Chlordiazepoxide
combined (EtOH)
Varied: some
Enhances frequency
anticonvulsants, muscle Overdose similar to EtOH
GABA binding to
relaxors in addition to intoxication; all
receptor --> Cl- influx
anxiolytic/sedative/ can develop dependence
resulting in
hypnotics
hyperpolarizatioin
Varied: some
Clonazepam Enhances frequency
anticonvulsants, muscle Overdose similar to EtOH
GABA binding to
relaxors in addition to intoxication; all
receptor --> Cl- influx
Diazepam (Valium) anxiolytic/sedative/ can develop dependence Oral form for kids
resulting in
hypnotics
hyperpolarizatioin
Lorazepam (inhibitory effect in
brain)
Oxazepam GABA must be
present to show any
effect (cannot affect Cl- Daytime sedation, Long-acting active
Flurazepam conductance alone) Nightmares metabolite
For staying asleep
Temazepam

Daytime anxiety,
Triazolam For starting sleep Shorter-acting
morning insomnia
Hasten recovery, Also antagonizes
Flumazenil BZ receptor antagonist
overdose zolpidem and zaleplon

Also used for Panic disorder, Enuresis, Chronic No CNS stimulation for
Drugs for Depression
pain, Eating disorders, Attention Deficit disorder normal patients
MAOa = NE, 5-HT
Monoamine Oxidase Inhibitors Nasty drugs
MAOb = DA

Phenelzine Low TI; hypotension,


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

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Tricyclic Antidepressants

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

High TI (death only with Requires downregulation


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

Other Antidepressants

Bupropion

Inhibits presynaptic
Mirtazapine
alpha 2 receptors

Trazodone Blocks reuptake of 5-HT

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Inhibits reuptake of NE
Venlafaxine
and 5-HT
Nefazodone

Maprotiline Inhibits reuptake of NE

Hypothalamic-Pituitary Drugs

Bromocriptine Excess Prolactin


Block prolactin (and GH)
production
Cabergoline Excess Prolactin and GH Long-acting; DA agonist

Chorionic Can induce ovulation,


Acts like LH
gonadotropin (hCG) steroidogenesis
Stimulates LH/FSH Diagnostic tool - locate
Gonadorelin (GnRH)
when pulsed problem of HP-axis Inhibit LH/FSH if given
Long-acting GnRH Too much E2/Test. - Endometriosis, uterine continuously
Leuprolide (Leupron)
agonist (less LH/FSH) fibroids, precocious puberty, prostate cancer
From urine of
Menotropins (hMG) Mostly FSH (some LH) In Vitro clinics
postmenopausal women
Blocks GH production
Octreotide
(acts like somatostatin)
Stimulates GH Diagnostic tool - can
Sermorelin (GHRH)
production by pituitary they make GH?

Somatropin GH analog By recombinant DNA

GnRH receptor
Abarelix Prostate cancer
antagonist

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous


Thyroid Drugs

Stimulates cellular Hypothyroid Long T1/2 (7 days)


Levothyroxine (T4)
metabolism when -->T3 (Hashimoto, Lithium)
Propylthiouracil Blocks organif. of I and Inhibits thyroid hormone
Hyperthyroid (Graves) Can cross placenta
(PTU) coupling of iodotyrosine synthesis (not I uptake)

Adrenal Drugs/Hormones Mostly Non-adrenal

Hydrocortisol Cannot bind to aldosterone receptor due to actions


Glucocorticoid
(cortisol) of 11beta-HSD-2 --> cortisone (inactive)
Converted to cortisol
Cortisone Many uses
(11beta-HSD-1)
(Hypofxn=Addison's,
Adrenal suppression
Betamethasone fetal lung maturation)
(must taper drugs when Long-acting; Only have
discontinuing), glucocorticoid effects;
Dexamethasone hyperglycemia, used to test axis
hypertension/Na
Prednisolone Synthetic glucocorticoids Acts like cortisol retention, edema,
Iatrogenic Cushings
Converted to
Prednisone Intermediate-acting
Prednisolone

Triamcinolone

Synthetic 20x more mineralC. vs.


Fludrocortisone
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

Selective estrogen
Tamoxifen Binds to receptor
receptor modulator
Breast cancer
Anastrozole
Aromatase inhibitors
Letrozole

Ovulation for ppl with


Clomiphene Ovulating inducing agent
polycystic ovarian dis.

Finasteride Blocks 5alpha-reductase


Prostate cancer
Androgen receptor
Flutamide
antagonist
Selective estrogen Acts only on bone
Raloxifene Prevent bone loss
receptor modulator receptors (not others)

Pancreatic Drugs/Hormones

Insulin Lispro Recombinant insulin

Sulfonylureas (1o)
Act on K+ channel to Disulfiram-like rxn
(Glyburide)
make B cell release Type II diabetes Short-acting; target
insulin Hypoglycemia, Drug
Repaglinide post-prandial glucose
interactions (EtOH)
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
Glucosidase inhibitor -
Acarbose Flatulence
reduces uptake frm gut
Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Drugs of Abuse

Beta 1, alpha, releases


Amphetamine
NE and DA
Methamphetamine
"speed"

Caffeine

Blocks DA reuptake (also CV, psychosis, lowered


Cocaine
NE) seizure threshold

Ephedrine

Methylphenidate

Phentermine

Sibutramine

CNS depressant (GABA, Alcoholic hallucinosis W/drawl CAN be fatal -


Ethanol Na, NMDA, 5-HT3???) Social
(DT's), suppressed ADH CV collapse from ANS
Converted to form- Treated with EtOH to
Methanol Acidosis, coma, death
aldehyde --> formic acid compete with enzyme

Ketamine

Lysergic acid NO withdrawl syndrome;


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

Mescaline Psychedelic NO withdrawl syndrome


Inhibit NMDA channels,
Phencyclidine (PCP)
block reuptake DA, NE
G-protein receptor in
Marijuana (THC)
CNS

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Appetite stimulant, anti-


Dronabinol Cannabinoid (THC)
emetic, anticonvulsant
Heroin (and other Probably involves G-
Withdrawl NOT fatal
opioids) protein, cAMP
Nicotinic and
Nicotine
dopaminergic pathways
Barbiturate-general CNS
Pentobarbital Withdrawl CAN be fatal
depression
Inhibits aldehyde Negative reward for OD can lead to CV Like metronidazole,
Disulfiram
dehydrogenase EtOH intake collapse from aldehyde sulfonylureas, cephs, etc
Opioid antagonist
Naltrexone
(mainly at mu receptrs)
Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

"Breaking phenomenon" Some allergies to sulfur Passive Na exchange Increase LDL, TGs, and
Thiazide Diuretics
with all Na excretors in structure distally can --> K loss total cholesterol

Hydrochlorothiazide 1o: Blocks NaCl Caution with renal


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

Loop Diuretics (High-Ceiling) Vasodilation following IV

Furosemide
Hypovolemia,
1o: Inhibit Na,K,Cl
hypokalemia,
Ethacrynic acid symporter in thick Edema, acute renal
hypocalcemia,
ascending limb failure, hypercalcemia, Also INCREASE Ca2+ in
hyperuricemia,
2o: inhibit NaCl chemical intoxication urine
Bumetanide ototoxicity (esp. E.
symporter in distal (increases excretion)
acid), impaired platelet
tubule
aggregation
Torsemide

Weak diuretics, usually given with thiazides to


Potassium-sparing Diuretics
prevent hypokalemia
Amiloride
(more potent) hyperkalemia, Lack of Na in cell to
Inhibit Na reabsorption CHF (3rd-line), cirrhosis
gynecomastia, loss of exchange prevents
in collecting duct w/ ascites, nephritic
libido, impotence, excretion of K
syndrome, HTN,
menstrual irregularities,
1o aldosteronism
leg cramps
hyperkalemia, Lack of Na in cell to
Inhibit Na reabsorptionCHF (3rd-line), cirrhosis
gynecomastia, loss of exchange prevents
in collecting duct w/ ascites, nephritic
Triamterene libido, impotence, excretion of K
syndrome, HTN,
menstrual irregularities,
Aldosterone antagonist 1o aldosteronism Also inhibits synthesis of
Spironolactone leg cramps
(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 Increase GFR, reduce Minor diuretics


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

Xanthines

Aminophylline Combined with other


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

Diuretics

Hydrochlorothiazide
See above
Furosemide

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Beta-adrenergic Antagonists

Propranolol
Reduce CO, and plasma
Metoprolol renin activity; also Cardiosensitive (Beta1)
Bronchoconstriction
inhibit presynaptic beta HTN
(except with metoprolol)
Nadolol receptors, CNS effects,
PNS effects
Pindolol

Alpha-adrenergic Antagonists

Decreases LDL, and total


Prazosin Alpha-1 blocker HTN, BPH
cholesterol

Inhibitors of Renin-Angiotensin System

Renal failure Non-peptide (orally


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

Centrally-acting Drugs

HTN, insomnia, opiate Decreases LDL, and total


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

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Combined therapy with diuretics & beta blockers


Vasodilators
to prevent adverse reflexes to vasodilators

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

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

Activation of ATP-
Minoxidil
sensitive K channels
Ca channel blocker,
Hydralazine Preeclampsia
inhibits enzymes ->ROS
arteriolar dilation, also
Fenoldopam Dopamine (D1) agonist Hypokalemia
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
Ibuprofen (and Reversible inhibition of control, antipyretic
wall
other 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
Binds to IIb/IIIa During & after coronary Hemorrhage,
Abciximab Monoclonal antibody
adhesion molecule artery procedures thrombocytpenia

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Xanthine derivative, Obstructed arteries,


Pentoxifylline
prevents claudication vascular dementia

Ticlopidine TTP, neutropenia, less


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

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
Also caused by diet, bowel dx, liver/bile dx
Vitamin K Prevent synthesis of II,
(reduced synthesis); Pregnancy (inc. clot
Antagonists VII, IX, X, proteins C, S
factors)

Inhibitors of Clotting Factors


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

Enoxaparin Low molecular weight


Less capacity to bind
Heparin - inhibit factor Higher bioavailability,
platelet, plasma
Dalteparin, Xa (less activation of Anticoagulation, DVT longer half-life
proteins, or osteoblasts
Ardeparin antithrombin III) prophylaxis, PE
Indirect inhibitor of Xa NOT assoc w/ low Does not bind to platelet
Fondaparinux
synthesis platelets or osteoporosis factor 4

Binds to Heparin- Reversing Can be used for Heparin


Protamine Sulfate
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
Synthetic thrombin
Ximelagatran Hemorrhage Oral
inhibitor (reduces fibrin)
Inactivates thrombin Hereditary AT-III Dizziness, chest pain,
Antithrombin III
(Iia) 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) Convert plasminogen Dissolution of formed other sites (advantage) plasminogen on fibrin
to active plasmin clots, evolving MI
Convert plasminogen Dissolution of formed
to active plasmin clots, evolving MI
Urokinase

Anistreplase Complex of others

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

Antifibrinolytic Agents (Preserves clots)

Lysine analog; inhibits


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

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Inhibit proliferation of smooth muscle into lumen


Stents with Anticoagulation Properties
of stent
Inhibit cell growth;
Sirolimus
anti-inflammatory
Stents
Inhibits phases of cell
Paclitaxel
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 Ach node) arrythmias increase catecholamines
Tachyarrythmias (NOT Potent, but questionable
Milrinone increaes Ca influx CHF (IV)
bradycardia) efficacy
Beta 1 agonist CHF (fixed, high grade Increases CO, and
Dobutamine
(Enantiomers-some 'a') coronary occlusion) decreases VFP
Carvedilol, Reduce SNS effects in
Beta blocking activity
Metoprolol CHF
Nesiritide (Brain Activates cGMP,
CHF (IV) Is NOT arrhythmogenic
natriuretic peptide) Increases GFR

Anti-Arrythmic Drugs

Class 1A

Atrial, AV junction, Hypotension, syncope IV; Anti-muscarinic


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

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Class 1B

IV; ineffective in normal


Lidocaine 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 Oral form of lidocaine
channels, slow Phase 0
When other 1B's don't Agranulocytosis, aplastic Oral form of lidocaine;
Tocainide
work anemia, int pneumonitis requires CBC monitoring

Class 1C
Long-term Na blocker, Proarrythmic effects,
Propafenone
slows all conduction Granulocytosis, SLE-like
Long-term Na blocker, Life-threatening V.tach Decreased ionotropy, Oral; No anti-muscarinic
Flecainide
increased threshhold ONLY CHF, V.tach, Torsades Inc [] w/ Amiodarone
Binds to Na channels in Proarrythmias, CHF,
Moricizine No anti-muscarinic
open state (lowrs Vmax) neurologic effects, shock

Class 2 (Beta blockers)

Blocks B1 and B2; dec


Propanolol IV more effective
CO, -ionotropy, slow AV
Conditions where
Sinus bradycardia from
Acebutolol More selective for B1 catecholamine excess is
dec. slope of phase 4,
responsible for
AV dissociation, rapid
Short-acting B1 blocker generating autonomous
Esmolol removal can cause fatal
for after cardiac surgery ectopic rhythm
disturbances,
(Pheocromocytomas,
Labetalol Bronchospasm,
exercise-induced
hypotension
Both Beta and A1 block V.tach), A.tach, PVC's
Carvedilol Free radical scavenger

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Class 3

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


Bretylium
prolongs AP, ERP (old) rapid IV enlrgemnt, HTN in some
Na block, K block, Ca SV/V.tach, also WPW Pulmonary fibrosis, Active metabolite, NOT
Amiodarone
block, a/b block (major DOC) corneal deposits, thyroid reverse rate dependent
Beta blocker, increases
Sotalol SV/V.tach Bradycardia, Torsades Reverse rate dependent
AP & ERP in all tissues
Prolongs AP & ERP (Na Afib, Aflutter (better at Will not depress cardiac
Ibutilide Torsades
channel agonist?) re-entry arrythmias) function; NOT RRD
Blocks rapid comp. of K Never together with
Dofetilide Afib, Aflutter Better in Atria, RRD
delayed rectifier channel Verapamil
K channel blocker,
Azimilide Afib LOW Torsades NOT RRD
prolongs AP, ERP

Class 4

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

Unclassified Anti-Arrythmic Agents

Reducing ventricular Abnormal reentries (worse with hypokalemia),


Digoxin Reduced AV conduction
response to Afib/flutter treated with lidocaine
K channel (A1) opener, Treating SV.tach, RAPID half-life (10sec); antagonizes
Adenosine
works in the nodes NOT Afib/Aflutter/Atach catecholamines, Diagnostic for SV.tach vs. V.tach
Anti-muscarinic: allows Bradycardias following
Atropine
SNS to dominate MI's or Vasovagals
2 or 3o heart block, Tachycardia, angina,
Isoproterenol Beta 1 and 2 agonst
Stokes-Adams attacks tachyarrythmias

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

May be combined with


Vasopressin Enhanced perfusion Vent. Fibrillation
epinephrine
Blockade of Ca, Na, K DOC for Torsades de Contra in complete heart
Magnesium
channels, ATPase pump Pointes block, renal failure
Hypokalemia, Torsades
Potassium
if Mg not working
Drugs for Hyperlipidemia

Inhibits mobilization of Inhibit VLDL synthesis, Gastric probs, Diabetes,


Nicotinic acid (niacin) 100% bioavailability
free fatty acids (FFAs) induce LPL; inc. HDL mylgia, rhabd., flushing

Lovastatin Also: plaque stability,


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

Inhibits cholesterol Gall stones? Inc. hepatic Eliminated via


Ezetimibe (Zetia) Often used with statin
absrp. (at brush border) enzymes; hedche, URIs glucoronidation

Cholestyramine
Bile acid sequestrants - Rash, fecal impaction, Increase hepatic LDL
prevent enterohepatic constipation receptors (need
Cholestipol
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 Fibrates
induce LPL, inc. HDL myalgia, rhabdo. (esp
proliferators-activated (fibric acid
Decrease with HMG-CoA inhib. &
Clofibrate receptor alpha (PPARs) derivatives)
triglycerides niacin)

Dietary Fiber Lowers cholesterol

Decreased hepatic synthesis of fats and VLDL


Fish oil (Omacor)
Decreased platelet aggregation

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Drugs for Ishemic Heart Disease (Antianginal)

Stimulate guanylate Relaxes smooth muscle Headache, syncope, Tolerance after 24 hrs to
Nitroglycerin (GTN)
cyclase --> Inc. cGMP Antiplatelet; Abort MI flushing patch method
Vasodilator (arteries and Stable angina
Isosorbide dinitrate
veins) (also GTN)
Minimal reflex
Diltiazem Ca channel blocker
sympathetic activation
HTN, angina, arrythmias
Ca channel blocker Headache, flushing,
Verapamil
(L type) constipation, dizziness
Ca channel blocker Prinzmetal's angina,
Nifedipine 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

Antiplatelet effects
Ticlopidine 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)

Nausea, upper
Iron Deficiency
Oral Iron supplement abdominal pain,
(Anemia)
Ferric Gluconate Liquid form(Floradix):
(Floradix) better/faster absorption

Fe Fumarate Nausea, upper 33% iron


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

Fe Ammonium
16.5% iron
Citrate
Iron Protein Absorp. NOT affected by
Succinylate H2 antag, drugs, food
Biproduct of sugar cane
Molasses Source of iron
processing
High risk of
Iron Dextran Anaphylaxis (need test
Hemodialysis w/ EPO, dose)
Injection site rxns,
Ferric Gluconate Abnormal absorption,
IV iron supplement Diarrhea, nausea,
(Ferrlecit) intolerance to oral, oral Preferred due to less
Anaphylaxis
Iron Sucrose noncompliance adverse effects
(Venofer)

Deferoxamine Iron chelator Iron toxicity (overdose)

B12 deficiency (inc.


Cyanocobalamin IM B12 injection Cold abscesses Very painful
methylmalonic acid)
NO B12 toxicity (for all
Methyl Cobalamin Sublingual B12
methods)
Deficiency/Prophylaxis To prevent neural tube
Folic Acid Oral, IV, IM, SC
in pregnancy defects
Procrit, Epogen Chronic renal failure, CV events, HTN, Iron supplement likely
(epoetin alpha) EPO analogs- induce AZT pts (suppress BM), seizures, thrombosis (all forms)
Aranesp RBC maturation Chemotherapy pts, (esp. renal failure); also Longer T1/2, lower
(darbepoetin alpha) Chronic inflammation Abuse potential! 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 Chemo in AML patients Better tolerated than
(Neupogen) Recombinant G-CFS -> Bone pain, splenic
(>55yo), BM transplant, GM-CSF, Neulasta
neutrophils/granulocytes rupture, ARDS from
PEG-Filgrastim to prevent neutropenia prolonged action (slow
(NO macrophages) neutrophil infiltrate lung
(Neulasta) (infections) renal clearance)

Hematide Stimulates EPO


In clinical trials
EPO receptor agonist
CERA
(long lasting)

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous


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

PGE1 Patent Ductus arteriosis


Alprostadil
Erectile Dysfxn

PGE1 analog Stimulates contraction


Misoprostol NSAID-induced ulcers Can cause abortion
--> preterm labor

PGE2 Abortion in combo w/


Dinoprostone Abortion, Induced labor
Misoprostol and MTX

PGI2 (Prostacyclin) Pulmonary HTN Mainly in endothelial


Epoprostenol Inhibits Platelet agg
(emergency) cells

Prostaglandin F2a PGF2a

Carboprost PGF2a analog Off US market

Glaucoma (topical) -
Latanoprost PGF2 analog
increases humor outflow
TXA2 (Inc. IP3 --> Inc Mainly in platelets - in
Thromboxane Promotes Platelet agg
Ca2+ --> vasoconstrict) response to injury

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)

Constricts Bronchi (H1) CNS neurotransmitter


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

1st Gen. Antihistamines

Diphenhydramine Minor Allergic reactions


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

2nd Gen. Antihistamines

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

Converted to Allegra via CYP inhibitors


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

H2 Receptor Antagonists

Cimetidine
(Tagamet)

Ranitidine (Zantac) Block H2 - Decrease


gastric acid secretion GERD, Ulcers
Famotidine (Pepcid) (volume and acidity)

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

5-HT1 agonists TREAT current migraine Treatment aimed at


Drugs for Migraines
5-HT2 antagonists PREVENT future ones vasoconstriction
Partial agonist (alpha Migraines, cluster Ergotamine, caffeine,
Ergot alkaloids
and 5-HT) - vasoconstric headaches dihydroergotamine
5-HT2 antagonist All prophylactics require
Methysergide Prophylaxis
(prevent vasoconstrctn) weeks to be effective
5-HT1D agonist (reverse Terminate acute Also (naratriptan,
Sumatriptan No dependency risk
vasodilation) migraine rizatriptan, zolmitriptan)
Propanolol (and Beta blocker - may have
Prophylaxis Dec platelet agg
other B blockers) action at 5HT receptors
Diltiazam, nifedip- Ca channel blockers - Prophylaxis of Dec frequency, little
Migraine-like headaches
ine, verapamil may involve 5HT receps migraines, clusters effect on severity
Prophylaxis of chronic
Lithium carbonate
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)


High dose (0 order); High dose -> uncouples
oxidative phosphorylation -> Hyperventilation
Fever, headache,
Inhibit COX - ASA irrev. and respiratory alkalosis; dose can ->
myalgia, neuralgia,
All others reversibly... acidosis; Gastric bleeding (->Fe def?), GI
Salicylates (Aspirin, dysmenorrhea,
Blocks probs, Ulcers?, Salicylism: tinnitus, hache, N/V,
etc) osteoarth., rheumatoid,
TXA2 required for dizzy, vision High frequency hearing loss
prophylaxis for heart,
platelet aggregation (reversible), Lipooxygenase activation may ->
Gout (high dose)
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-
inflammatory, Low GI, NOT an NSAID
No effect bleeding/resp Peroxides->Inactive
Not uricosuric Can affect ASA
Acetominophen Weak inhibitor of COX Analgesic, Antipyretic
Hepatic necrosis binding Greater effect
(esp. EtOH, fasting) in CNS? Free radical
Renal tubular metabolite
necrosis

Celecoxib (Celebrex) Selective COX-2 Contains Sulfa


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

Same as ASA (better for GI (N/V), CNS - dizzy, Cross sensitive ASA
Ibuprofen COX inhibitor (NSAID)
dysmenorrhea) headache, etc. Naproxen - long acting
Intractable fever Sulindac - prodrug with
COX inhibitor (Most (Hodgkins), ankylosing Frontal headache, GI less toxicity
Indomethacin
potent one) spond., OA, RA, GoutA ulcers, blood loss Contraindicated: Ulcers
close patent ductus Pregnancy, Psychiatric
Short-term analgesic Only IM NSAID
Ketorolac COX inhibitor Hepatic, renal toxicity
(compare opioids, etc) No evidence of abuse

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Diflunisal NO antipyretic Poor entry to CNS

Accumulates in synovial
Diclofenac
fluid - rapid onset

Etodolac Similar to indomethacin

Prodrug, ketone ->


Nabumetone
acetic acid derivative
COX inhibitors (NSAIDs)
May also block PG
Meclofenamate
receptors
Piroxicam
(and other "- Long T1/2
cams")
May be better tolerated
Tolmetin
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 SAARDs
(Plaquenil) Retinal damage-elderly
Mild RA
Sulfasalazine HA (G6PD), Naus, rash
(Azulfidine) Leukopenia, hepatitis
Moderate RA Hep.enzymes, Dec BM High response rate; Oral
Methotrexate (MTX)
(Often DOC) teratogenic, stomatitis weekly dose, FA supple
Infrequent (usually in Diarrhea, alopecia, hep. Less expensive, higher
Leflunomide (Arava)
combo with MTX) enzymes, teratogenic toxicities
Stomatitis, rash,
Gold (injectable) Weekly CBC and UA
proteinuria
Azathioprine Metabolized to 6-
Immunosuppresive
(Imuran) mercaptopurine
IL-1 antagonist If failure w/ TNF
Anakinra
Inhibits inflam effects inhibitors

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Soluble TNF receptor -


Etanercept
antagonizes TNF
Risk of serious infections Require TB screening
Infiximab
and lymphoma before use
Anti-TNF Monoclonal AB
Adalimumab

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

Decrease pain/inflammation, Dec phagocytosis of Initial Tx, or sub. for Indomethacin most
NSAIDs (NOT ASA)
urate crystals -> more excreted Colchicine common
Binds to tubulin, inhibits Acute Gout (1st line) - Reduces leukocyte
Colchicine Diarrhea, N/V
polymerization 12-24hrs till effect migration/inflammation
Inhibits Xanthine Oxids Chronic Gout (often in Prolongs T1/2 of 6-
Allopurinol Uncommon
Reduces uric acid syn. combo to start) mercaptopurine
Recombinant urate
Rasburicase 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
Triamcinolone receptors in lungs HTN

Ipratropium Br & Anticholinergic - blocks


Atropine M3 receptors

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

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

Epinephrine Most cardiac effects

Least cardiac effects,


Albuterol (more B2 selective)
Tremor

Terbutaline B-adrenergic agonists -


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

Fluticasone

Formoterol

Inhibits cellular actvaton Mast cell stabilizer, Inhibits eosinophil


Cromolyn Sodium
(Cl channels) inhibits cough infiltration
Most effective Few (sposed to liquify
Water Inhaled steam/vapor
expectorant bronchial secretions)

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

Splits disulfide bonds Bronchitis, COPD,


Acetylcysteine
-> less viscosity Acetominophen OD
Recomb. DNAase -> Cystic fibrosis, Chronic Cough, wheeze,
Dornase Aerosol
Cleaves mucus bronchitis hemoptysis, pharyng

Amrinone
Bronchodilation -
PDE3 inhibitors
Asthma
Enoximone

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Ipopamine

Milrinone Phosphodiesterase Nausea and vomiting


Bronchodilation -
Inhibitors --> may limit use of PDE4
Asthma
Vesnarinone Bronchodilation inhibition

Pimobendan

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

Zarfirlukast
Leukotriene receptor Food decreases
Antagonist (nonspecific) Increase theophylline bioavailability
Montelukast and warfarin
Met. by CYP2C9,3A4
5-lipooxygenase Headache, hep. toxic
Zileuton
inhibitor Dyspepsia
Headache, viral inf.,
Omalizumab Anti-IgE monoAb 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)
Proton-pump inhibitors
Rabeprazole
(PPIs)
Esomeprazole &
Pantoprazole

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Alkalosis when Last much longer when


NaHCO3
prolonged, UTI, gas given with food
Antacids - neutralize HCl
No alkalosis, rebound
CaCO3 (Tums) (Do NOT inhibit Non-systemic
acid hypersecretion
production)
Diarrhea, renal excretion (Mg)Most potent (Al)Low
Mg(OH)2, Al(OH)3
Milk Alkali syndrome phos, Alzehimer?
De-foaming action -
Simethicone Antiflatulent, GERD
coalesces gas bubbles
Cimetidine Headache, dizziness, GI, low sperm, gynecomstia,
(Tagamet) menstrual, halluc, agitation, apnea, renal failure
Lacks the hormonal 5x more potent than
Ranitidine (Zantac) H2-receptor antagonists adverse effects Cimetidine
(usually combo with Prevent ulcer
Famotidine (Pepcid Less hormonal and drug <160x more potent
antibiotics for H.pylori)
AC) interaction effects than Cimetidine
Similar to Ranitidine,
Nizatidine Does not inhibit P450
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
Contra: Above except
Pirenzepine (anticholinergic) 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
Small amount of Al Rare; may impair NOT in combo with
Sucralfate Mucosal Protection
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

Antidopamine - inhibits
Sulpiride NOT approved in US
gastrin release

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Persistent constipation, Cathartic colon syndrome, Addiction, Hypok+,


Laxatives (and Cathartics)
CV dz, hernia, parasites Malabsorption, Liver abnormalities (DSS)
PGE2->cAMP also
Castor oil 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 Irritant/Stimulant tumors; Others-colic bacteria (delay action)
Inhibit Na/K ATPase, laxative Carcinogen - Removed Must be absorbed
Phenolphthalein
Increase cAMP and PGE from market glucoronidated
Increase intestinal injury
Bisacodyl Increase K permeable Oral and rectal

Fiber-Hphilic colloids Cellulose fibers take up Few, requires LOTS of Also for acute diarrhea
(bran, psyllium, etc) water -> swell water (soak up water)
Polyethylene glycol
Isosmotic lavage Bulk forming laxatives Electrolyte solution
(PEG - GoLytely)
Saline (and other For evacuation before
Osmotic
salts) procedures
Inhibit Na/K ATPase
Docusate Minimal laxative effect
Increase cAMP
Glycerin
Stool softeners No salts present
suppositories
Mineral oil Leaks past anal
Fat Vitamin def.
(Liquid petrolatum) sphincter

Antidiarrheals

Diphenoxylate Analog of meperidine


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

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Absorbs toxins of E.coli, Black tongue/stools,


Bismuth salts Traveler's diarrhea
Decreases PG, cAMP Impaction

Kaolin Diarrhea
Thickeners and water
Kaopectate
binders
Pectin

Emetics and Antiemetics and GERD

Must enter CNS (delay)


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

N/V, Anorexia in AIDS For cancer-


Dronabinol (THC) Sedation, psychoactive
patients chemotherapy

Ondansetron Pre-Tx for


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

Chlorpromazine Inhibit DA, Ach, His, and Post-op and post-rad. Works in emetic center
(Phenothiazines) alpha receptors Nausea/vomiting (oral/IV/rectal)
Dopamine receptor D2 Increases tone of
Metoclopramide GERD Diarrhea
antagonist -> inc. tone esophageal sphincter
5-HT4 agonist Nocturnal heartburn Selective availability
Cisapride
(Indirect Ach agonist) (GERD), constipation NO effect on DA system

Drug/Class Mechanism Clinical Uses Side Effects Miscellaneous

Inflammatory Bowel Disease

Inhibit PG and Leukot. Upper GI irritation,


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

Anticholelithics

Prevents absorption of Also promotes


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

Irritable Bowel Syndrome (IBS)

5-HT4 agonist - Women w/ IBS w/ Heart attacks, stroke,


Tegaserod Removed from market
stimulates motility Constipation (shorterm) headache, diarrhea
5-HT3 antagonist - Women w/ IBS w/
Alosetron 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- NO CNS
Methanol poisoning
methylpyrazole) effects/depression
N-acetylcysteine
Acetaminophen OD
(NAC)

Desferoxamine Iron OD

Arsenic poisoning
Dimercaperol
(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

High lipids, HTN, ather- Induces CYP3A4, anti- Can cause bleeding w/
Garlic
osclerosis, Cancer thrombotic, antiplatelet surgery
Controversial
Echinacea Colds, Flu
effectiveness
Glucosamine Osteoarthritis, TMJ Does NOT affect insulin
Shellfish allergy
(sulfate) arthritis levels
(Panax) Ginseng Fatigue, "Adaptogen" Insomnia, Nervousness

Age-related macular
Lutein Carotenoid
degeneration (before)
Alzheimer Dz, Memory Interactions (CYP?), Some positive evidence
Ginkgo
enhancer, Claudication Seizures, Delayed onset for all 3 uses
Estrogenic (low) & Menopausal Sx, Breast Lymphocytopenia w/ Mech depends on
Soy
Antiestrogenic (high) Cancer certain derivative endogenous levels
Hepatotoxicity, Sedation CYP2D6 required to
Kava Anxiety (short term)
w/ other CNS depresnts metabolize
Prolonged anesthesia w/
Valerian GABA agonist Insomnia, Anxiety Additive sedation
surgery
No effect on PSA, Similar to finasteride
Saw Palmetto BPH (minor)
No impotence effectiveness
Depression (mild to 5-HT Syn. w/ SSRI's, Similar to TCA
St. John's Wort
moderate) Induces CYP effectiveness
Similar to NSAID
Chondroitin Osteorthritis Role in Prostate cz?
effectiveness

Black Cohosh Menopausal Sx Hepatitis (rare)

Coenzyme Q10

Sympathomimetic (like Weight loss ("Ephedra- Hemorrhagic stroke, Contains tyramine, is


Bitter Orange
phenylephrine, norepi) free") inhibits CYP3A4 similar to Ephedra
O3&mucus)