Drew's Medical Pharmacology

Front 1

Autonomic Exceptions:
Adrenal Medulla
Sweat Glands
Renal Vasodilator fibers

Back 1

epinephrine
acetylcholine
dopamine

Front 2

Catecholamine synthesis pathway

Back 2

tyrosine
(tyr hydroxylase) (rate lim)
Dopa
(aromatic L-aa decarboxylase)
Dopamine
(Dopamine beta hydroxylase)
Norepinephrine
(Phenylethanolamine Nmethyl tranferase)
Epinephrine

Front 3

Metyrosine
(Action, Problems, Clinical Use)

Back 3

Action: tyrosine hydroxylase (competitive inhibitor), depletes catecholamines everywhere
Problems: Sedation/depression, crystalluria, GI upset (hypermotile, diarrhea)
Clinical Use: Pheochromocytoma (b/f surg)

Front 4

facilitates false transmitter formation

Back 4

promiscous decarboxylase, DbH

Front 5

false transmitter

Back 5

any substance capable of being stored and released in place of the substance normally serving as the transmitter in a given neuron.

Front 6

Methyldopa (Aldomet)

Back 6

Action: centrally acting false transmitter, decreases sympathetic nervous activity in brain, decreases vasoconstriction
Problems:
Clinical Use: antihypertensive (centrally acting)

Front 7

Guanethidine

Back 7

Action: adrenergic neuron blocker, blocks vesicular release
Problems: cardiac depression, gi upset, orthostatic hypotension
Clinical Use: obsolete, antihypertension

Front 8

Reserpine

Back 8

Action: blocks VMAT, depletes stored NE
Clinical Use: antihypertensive (periph and central)
Problems: periph: cardiac depression, orthostatic hypotension, GI upset)
central: sedation, SEVERE DEPRESSION (contra depr)

Front 9

Cocaine

Back 9

Action: Uptake I blocker
Clinical Use: topical local anaesthetic during surg (nasal mucosa, lacrimal ducts)(vasoconstriction min bleeding)
Problems:adverse peripheral effects: increased BP, HR (stroke, arrhythmias, MI, sudden death)

Front 10

Imipramine

Back 10

Action: Uptake I blocker
Clinical Use: tricyclic antidepressant
Problems:

Front 11

MAO

Back 11

monoamine oxidase
oxidizes amine to aldehyde
nerve terminals, liver, kidney, gut mucosa and flora

Front 12

MAO-I

Back 12

Action: inhibit MAO
Clinical Use: antidepressants, parkinson's
Problems: "wine and cheese" syndrome

Front 13

COMT

Back 13

catechol-O-methyl transferase
adds methyl to -OH on a monoamine
liver

Front 14

COMT inh

Back 14

entacapone
adjunct in parkinsons tx

Front 15

Wine and Cheese Syndrome

Back 15

MAO inh with Tyramine
Tyramine acts as indirect sympathomimetic
Result: HYPERTENSIVE CRISIS
normally rapidly degraded by MAO
tyramine found in beer, wine, cheese, processed meats

Front 16

Key to specificity in autonomic drugs

Back 16

multiple types of adrenergic receptors

Front 17

Epi Reversal

Back 17

Phentolamine (alpha blocker) causes unmasking of beta action of Epinephrine, allowing Epi to cause a decrease in blood pressure.

Front 18

Norepinephrine
Receptors
Effects on:
pulse rate
BP
TPR

Back 18

Alpha, Beta I only
pulse decrease (baroreceptor)
BP increase (incr TPR)
TPR increase (alpha)

Front 19

Epinephrine
Receptors
Effects on:
pulse rate
BP
TPR

Back 19

All adrenergic receptors
pulse increase (direct B1)
BP minor increase (dose dependant)
TPR decrease (B2 eff)

Front 20

Isoproterenol
Receptors
Effects on:
pulse rate
BP
TPR

Back 20

Beta agonist only
Pulse increase
BP minor decrease
TPR decrease

Front 21

Variables of blood pressure, eq

Back 21

BP=COxTPR
Baroreceptor reflex
Vagal dominance

Front 22

alpha 1 activity

Back 22

vasoconstriction (innervated)
pupillary dilation
ejaculation
inh micturition
GI inhibition

Front 23

alpha 2 activity

Back 23

vasoconstricion (uninnervated)
prejunctional inh of NE release

Front 24

beta 1 activity

Back 24

cardiac stimulation (innervated)
secretion of renin

Front 25

beta 2 activity

Back 25

cardiac stimulation (unninervated minor)
vasodilation (uninnervated)
bronchodilation
uterine relaxation
GI inhbition
Glycogenolysis (Liver)

Front 26

Epinephrine

Back 26

Action: potent agonist at all alpha and beta receptors
Clinical Use: anaphylaxis, cardiac arrest; adjunct w/ local anaesthetics (vasoconstriction); bronchodilator (primatene mist)
Problem: pharmacokinetics (rapidly degraded)
NEVER: fingers toes, penis, nose (vasoconstrict to necrosis)
Problem:

Front 27

Alpha agonists

Back 27

Sympathomimetic pressors.
Clinical Uses:
1. Nasal decongestants
2. adjunct local anaesthetics
3. Maintenance of BP (spinal anaesthesia, shock)
4. tx PAT (paroxysmal atrial tachycardia
5. Eye drops (vasoconstrict vessels)
6. Mydriatic (dilates pupil)

Front 28

Phenylephrine

Back 28

Action: std alpha 1 agonist
Clinical Use: see alpha agonists

Front 29

Ephedrine, pseudoephedrine (SUDAFED)

Back 29

Action: direct agonist mostly beta, indirect agonist noradrenergic and CNS
Clinical Use: nasal decongestant (alpha direct and indirect)
Problems:MAOI potentiates effects, hypertensive effect
CNS: amphetamine like action, ephedra used as weight loss w/ adverse effects

Front 30

Ephedrine vs. Epinephrine

Back 30

kinetics: ephedrine resistant to MAO and COMT (orally active)
dynamics: Ephedrine 1)direct at beta 2)indirect on noradrenergic nerve endings in periphery and CNS

Front 31

Indirect Sympathomimetic - Mechanism

Back 31

1. uptakeI
2. vesicles, kicks out NE
3. some released NE inactivated by MAO
4.uptakeI running backwards, NE out, effect

Front 32

MAO-I inh rxn w/ IS

Back 32

MAO-I potentiates the efffects of indirect sympathomimetics by blocking the action of MAO on NE liberated from vesicles. Leads to hypertensive crisis.

Front 33

adverse effects linked to ephedrine/pseudoephedrine

Back 33

Indirect stimulation at alpha receptors causes
1. increased BP, stroke
2. Cardiac arhythmia, MI
3. CNS stim and seizure
(similar to amphetamine)

Front 34

Amphetamine
Methamphetamine
Ephedrine

Back 34

Mixed action Adrenergic agents
Used for appetite suppresant, narcolepsy, and ADHD.
Probs:
1. tolerance, abuse, and adverse reactions including:
cardiac arrhythmia, angina, stroke, psychosis, convulsions.

Front 35

Phentermine

Back 35

Ingredient in "Phen-Phen" appetite suppresant that was taken off the market because it causes heart valve damage.

Front 36

Methylphenidate (Ritalin)

Back 36

Amphetamine like CNS stimulant used to treat ADHD.
Not as effective as amphetamine(ADDERALL), but fewer side effects.

Front 37

Imadazoline-type alpha receptor agonists (topical)

Back 37

Used topically as nasal decongestants and in eye drops (ex: visine). Topical therapeutic effects from vasoconstriction.

Front 38

Imadazoline-type alpha receptor agonists (systemic)

Back 38

Centrally acting antihypetensives
Ex: Clonidine
Brimonidine

Front 39

Clonidine

Back 39

centrally acting Imadazoline-type alpha receptor agonist
used as an antihypertensive.
Alpha2 receptor agonist acts in brainstem to decrease sympathetic nervous system activity to heart and blood vessels. Problems: sedation, dry mouth, WITHDRAWAL syndrome with prolonged use.

Front 40

Brimonidine

Back 40

centrally acting alpha agonist
decreases secretion of intraocularr fluid in glaucoma

Front 41

Clonidine Withdrawal syndrome

Back 41

alpha2 stim results in DECREASED symp activity and lowers BP and Hr. abrupt withdrawal after prolonged use results in hypertension, tachycardia, angina, or MI due to relatively lowered amounts of alpha2 receptors in brain.

Front 42

Labetalol

Back 42

Competitive antagonist of α & β receptor (sympathetic antagonist)
Affect heart and blood vessels
Tx: HTN & clonidine withdrawal

Front 43

Albuterol

Back 43

β-2 selective agonist (bronchodilate)
ORAL drug (COMT can't degrade)
Tx: "rescue" asthma

Front 44

Salmeterol

Back 44

β-2 agonist (bronchodilate)
Long acting (slow onset)
Tx: "control" asthma (NOT rescue)

Front 45

Ritodrine

Back 45

β agonist (β2>β1) - uterine relaxation
Tx: premature labor
Probs: tachycardia if interact w/ β1

Front 46

Dobutamine

Back 46

β1-agonist (also β2 and α)
Affect ionotropic > chronotrophic
Tx: cardiac failure (acute emergencies), laboratory stress test
Probs: IV only (systemic) - arrhythmogenic

Front 47

Dopamine

Back 47

D1 agonist (vasodilate kidney vessels), some α & β agonist activity, some indirect sympathomimetic activity (ISA)
Tx: Shock (maintain kidney perfusion), CHF
Probs: IV only

Front 48

Phentolamine

Back 48

Competitive α-blockers
Probs: non-selective

Front 49

Phenoxybenzamine

Back 49

Irreversible (non-competitive) α-blockers
Tx: pheochromocytoma
Probs: Non-selective (accentuate cardiac stimulation), MI, arrhythmia,
NOT GOOD 4 HTN

Front 50

Prazosin

Back 50

α1-antagonist (↓ TPR, ↓ sympathetic stimulation of smooth mm)
Tx: BPH, CHF, HTN
Probs: First dose phenomenon, hypotension, syncope

Front 51

Tamsulosin

Back 51

α1-antagonist
VERY selective for urinary flow (low incidence of orthostatic hypotension)
Tx: BPH

Front 52

Propanolol

Back 52

Competitive β-blocker (depress membrane excitability)
Reduce Cardiac Output
Tx: HTN, angina, arrhythmia, ischemic heart disease
Probs: "1st pass effect" (pharmkinetic), heart failure, bronchoconstriction (bad 4 asthma), hypoglycemia, CNS effects (sedation, insomnia, etc)

Front 53

Metaprolol

Back 53

Competitive β1-blocker (β1>β2 = cardioselective)
Tx: HTN, angina, arrhythmia, ischemis heart disease, CHF
Probs: short 1/2 life (3-4 hrs)

Front 54

Nadolol

Back 54

β-blocker (NOT selective)
Tx: HTN, CHF
Renal degradation
Longer 1/2 life (10-24hrs)

Front 55

Atenolol

Back 55

β1-blocker (cardioselective)
Tx: HTN, CHF
Renal degradation
Longer 1/2 life (10-24hrs)

Front 56

Pindolol

Back 56

Partial agonist (all β-receptor)
Intrinsic Sympathomimetic Activity
Tx: HTN, CHF
Benefit: less cardiac depression, less bronchoconstriction, huge ↓ in TPR

Front 57

Esmolol

Back 57

β-blocker (cardioselective)
EXTREMELY short 1/2 life (5-10min)
Tx: Protect heart from catecholamine during surgery
Give by infusion

Front 58

Carvedilol

Back 58

β-blocker
Tx: CHF
Reduce mortality and morbidity in CHF
"start LOW, go SLOW"

Front 59

Botulinum Toxin

Back 59

Prevent exocytosis of ACh (at neuromuscular jx and cholinergic nerve)
Tx: dystonia, cerebral palsy, occular mm spasms, anal fissure, hyperhydrosis, cosmetic uses
LOCAL ADMIN. ONLY

Front 60

Muscarine

Back 60

Ach agonist at muscarinic receptors (cardiovascular, glands, smooth mm)
Enhance parasympathetic action
"Fast Mushroom Poisoning"

Front 61

Pilocarpine

Back 61

Muscarinic agonist
Tx: open angle glaucoma (topically-drain interoccular fluid), dry mouth (Sjogren's, radiation)-systemic

Front 62

Bethanechol

Back 62

Muscarinic agonist (ACh analog)
RESISTANT to cholinesterase
Tx: urinary retention (GI stimulation)
Probs: cardiovascular & respiratory effects
Contra: Asthma, peptic ulcer, coronary insufficiency
NEVER give IV or IM

Front 63

Methacholine

Back 63

Muscarinic agonist (ACh analog)
RESISTANT to cholinesterase
Use: bronchoconstriction - provocative test for asthma
Probs: cardiovascular & respiratory effects
Contra: Asthma, peptic ulcer, coronary insufficiency
NEVER give IV or IM

Front 64

Atropine

Back 64

Muscarinic antagonist (block PSNS)
NO EFFECTs on blood vessels
Tx: cardiac arrest, nerve gas poison
Low dose - affect glands, eye, etc..
High dose - affect CNS (anti-motion sickness, anti-Parkinsons)
Probs: dry mouth, hyperthermia (kids), exacerbation of glaucoma, urinary retention (old), confusion, coma, delirium
LACK selectivity

Front 65

Scopolamine

Back 65

Muscarinic-antagonist - lipophillic (more CNS action)
Tx: motion sickness (transdermal)
Probs: dry mouth, blurred vision sedation, confusion/psychosis @ high dose

Front 66

Ipratropium

Back 66

Muscarinic-antagonist (similar to atropine)
Tx: asthma, COPD
Probs: hypotension, muscle weakness @ high dose, poor absorb
Use in combo w/ albuterol

Front 67

Tolterodine

Back 67

Muscarinic-antagonist
NO selectivity
Tx: overactive bladder
Probs: dry mouth, constipation

Front 68

Nicotine

Back 68

Nicotinic-agonist
NO selectivity
Tx: smoking cessation (low dose)
Probs: ADH release, stimulate SNS, block neuromuscular, block GI/glands
Depolarization Blockade
Toxicity: convulsion, coma, HTN, arrhythmia, neuromuscular failure

Front 69

Varenicline

Back 69

Nicotinic receptor partial agonist (CNS):
1. Release of dopamine (low-med) @ reward center-mimic nicotine effect
2. Block binding of nicotine
Tx: smoking cessation
Prob: nausea, headache, constipation, abnormal dreams, mood changes

Front 70

Hexamethonium/Mecamylamine

Back 70

Ganglionic/nicotinic blocker
PARALYZE ANS
Tx: HTN, dissecting aortic aneurysm, autonomic hyperreflexia, hemorrhage in surgery
Prob: tachycardia, hypotension, dry mouth urinary retention, mydriasis, cycloplegia

Front 71

Edrophonium

Back 71

Competitive Cholinesterase Inhibitor - bind "negative" pocket & occlude active site (very brief!)
Use: Dx Myasthenia Gravis
TENSILONE test

Front 72

Physostigmine

Back 72

Substrate Cholinesterase Inhibitor
Carbamates (slow hydrolysis)
Enhance muscarinic, block nicotinic
Tx: Glaucoma, Alzheimer's, Myasthenia Gravis
Prob: GI upset

Front 73

Neostigmine

Back 73

Substrate Cholinesterase Inhibitor
Carbamates (slow hydrolysis)
Enhance muscarinic, block nicotinic
Tx: MYASTHENIA GRAVIS, paralytic ileus, bladder atony
Prob: GI upset, low bioavailability

Front 74

Echothiophate

Back 74

Substrate Cholinesterase Inhibitor
Organophosphate (permanent)
Enhance muscarinic, block nicotinic
Tx: Glaucoma
Prob: muscle weakness, respiratory failure, bradycardia, arrhythmia, asphyxiation, convulsions
DUMBELS & DEATH

Front 75

DUMBELS

Back 75

Signs of nerve gas (organophosphate) poisoining:
Diarrhea
Urination
Miosis
Bronchospasm & bradycardia
Emesis
Lacrimation
Salivation & sweating

Front 76

Sarin

Back 76

Substrate Cholinesterase Inhibitor
Organophosphate (permanent)
Enhance Muscarinic, Block Nicotinic
Military Nerve Gas - POISON
Use: DEATH
Counteract: Atropine + 2-PAM

Front 77

VX

Back 77

Substrate Cholinesterase Inhibitor
Organophosphate (permanent)
Enhance Muscarinic, Block Nicotinic
Military Nerve Gas - POISON
Use: DEATH
Counteract: Atropine + 2-PAM

Front 78

Parathion

Back 78

Substrate Cholinesterase Inhibitor
Organophospate (permanent)
Use: Insecticide
Prodrug (Paraoxon = active)
Humans-don't metabolize

Front 79

Malathion

Back 79

Substrate Cholinesterase Inhibitor
Organophospate (permanent)
Use: Insecticide
Prodrug (Malaoxon = active)
Humans-don't metabolize

Front 80

Pralidoxime (2-PAM)

Back 80

Anti-organophosphate intoxication
Act on: Nicotinic & peripheral Muscarinic
Tx: Nerve gas poisoning
MUST give w/ atropine - FAST
Worry about "aging" effects

Front 81

Drew & Nirav

Back 81

Have a good weekend