Pharm (Exam 1)

Front 1

Acetylcholine

Back 1

Choline Ester

Quickly hydrolyzed by AchE

Hint 1

Rapid miosis

Front 2

Bethanechol

Back 2

Choline Ester

Not hydrolyzed by AchE

Strong muscarinic activity

Hint 2

Acute postop & postpartum non-obstructive urinary retention
Neurogenic atony of urinary bladder
Adverse: generalized cholinergic stimulation

Front 3

Carbachol

Back 3

Choline Ester

Not hydrolyzed by AchE

Muscarinic & nicotinic

Hint 3

Intraocular miosis during surgery
Reduces intraocular pressure after cataract surgery

Front 4

Methacholine

Back 4

Choline Esterase

Hydrolyzed by AchE but slower

Predom muscarinic w/ slight nicotinic

Hint 4

Diagnosis of bronchial airway hyperreactivity w/ no apparent asthma

Front 5

Muscarine

Back 5

Natural alkaloid

Muscarinic receptor sites

Front 6

Arecoline

Back 6

Alkaloid

Muscarinic & nicotinic

Front 7

Pilocarpine (3 amine)

Back 7

Alkaloid

Hydrolyzed by AchE

Partial muscarinic

Hint 7

Agent for open angle glaucoma
Management for acute angle-closure glaucoma
Adverse: CNS disturbances; sweating & salivation

Front 8

Edrophonium (4 amine)

Back 8

Indirect cholinergic agonist

Binds reversibly to active site (2-10 min)

Hint 8

Diagnosis of myasthenia gravis
Reverse NM block from non-depolarizing muscle blockers

Front 9

Physostigmine (carbamate & 3 amine)

Back 9

Indirect cholinergic agonist

Covalent bond with enzyme (30 min - 6 hrs)

Hint 9

Overdose of anticholinergic drugs
Cross BBB and produce central cholinergic effects
(Not given TCA overdose due to depression of cardiac)
Adverse: convulsions; bradycadia; muscle paralysis

Front 10

Neostigmine (carbamate & 4 amine)

Back 10

Indirect cholinergic agonist

Covalent bond with enzyme (30 min - 6 hrs)

Hint 10

Reversal of non-depolarizing NM blockers after surgery
Treatment of myasthenia gravis (pyridostigmine used)
Prevention & treatment of postop distention & urinary retention
Adverse: cholinergic effects

Front 11

Echothiophate

Back 11

Organophosphate

Forms phosphorus-enzyme bond

Hint 11

Glaucoma

Front 12

Malathion

Back 12

Organophosphate

Thiophosphate insecticide

Converted to oxygen analogs

Hint 12

Metabolized to inactive products in birds and mammals

Front 13

Parathion

Back 13

Organophosphate

Thiophosphate insecticide

Converted to oxygen analogs

Hint 13

Not detoxified effectively in vertebrates

Front 14

Tabun, sarin, soman

Back 14

Nerve agents

Organophosphates

Front 15

Orally active inhibitors of AchE for Alzheimer's

Back 15

tacrine
donepezil
rivastigmine
galantamine

Front 16

Pralidoxime

Back 16

Can reactivate inhibited AchE

If given before ageing, can split phosphate-enzyme bond
Can be used as cholinesterase regenerator for insecticide poisoning

Hint 16

If exact agent is unknown and patient has toxicity, should be given empirically

Front 17

Atropine (3 amine)

Back 17

Muscarinic antagonist

SLUDGE (prevents)

Readily absorbed; partially metabolized by liver; eliminated in urine --> half-life: 4 hrs

Hint 17

Reverse excessive muscarinic effects

Adverse: See notes

Front 18

Scopolamine

Back 18

Similar to atropine but greater actions on CNS & longer action duration

Hint 18

Effective anti-motion sickness drug
Blocks short-term memory
Low doses - sedation; high - excitement

Used for mydriasis & cyclopegia

Front 19

Ipratropium (4 amine)

Back 19

Muscarinic anatagonist

Hint 19

Inhaled for asthma & COPD

Front 20

Tiotropium (4 amine)

Back 20

Muscarinic antagonist

Hint 20

Superior to ipratropium as bronchodilator for COPD

Front 21

Homatropine
Cyclopentolate
Tropicamide

Back 21

3 amine muscarinic antagonist

Hint 21

Mydriasis with cycloplegia --> preferred to atropine due to shorter action duration

Front 22

Benztropine
Trihexyphenidyl

Back 22

Muscarinic antagonist

Hint 22

Treats parkinsonism and extrapyramidal effects of antipsychotics

Front 23

Glycopyrrolate (4 amine)

Back 23

Antimuscarinic agent

Hint 23

Orally to inhibit GI motility
Parenterally to prevent bradycardia

Front 24

CONTRAINDICATIONS OF ANTIMUSCARINIC AGENTS

Back 24

Angle-closure glaucoma
Prostatic hypertrophy (increases risk of urinary retention)
Elderly

Hint 24

In elderly, hazardous to cognitive impaired: acute encephalopathy, falls, urinary retention, constipation, cognitive deficits

Front 25

Tubocurarine

Back 25

Nondepolarizing (competitive) blocker

Hint 25

Binds to nicotinic receptor and prevents Ach binding

Used for anesthesia to relax skeletal muscle

Given IV - no BBB crossing

Adverse: Autonomic effects (moderate blocking of M receptors); Histamine release

Front 26

Succinylcholine

Back 26

Depolarizing blocker

Flaccid paralysis (depolarizes and prevents repolarization)

Hint 26

IV by continuous infusion

Rapidly hydrolyzed by Ach-esterase

Brief duration of action and rapid onset

ECT & rapid endotracheal intubation

Adverse: Malignant hyperthermia --> most incidents occur from combination with this and halogenated anesthetic
Treated with dantrolene

Front 27

Hemicholinium-3

Back 27

Blocks CHT-1 (no uptake of choline for Ach synthesis)

Hint 27

Research tool

Front 28

Vesamicol

Back 28

Blocks VAchT (no storage of Ach into vesicles)

Hint 28

Research tool

Front 29

Botulinum toxin

Back 29

Prevents synaptic vesicle fusion with axon terminal membrane --> inhibits Ach release

Hint 29

Treats diseases with increased muscle tone: torticollis, achalasia, strabismus, blepharospasm, other focal dystonias

Front 30

Epinephrine

Back 30

Catecholamine

Low doses: B effects (vasodilation)
High doses: A effects (vasoconstriction)

Hint 30

Large dose: increased BP
Low dose: decreased BP
See notes

Uses: Anaphylactic shock; asthmatic attacks; anesthetics; glaucoma

Interactions: Hyperthyroidism; cocaine

Front 31

Norepinephrine

Back 31

A receptors most affected

Hint 31

See notes

Front 32

Dopamine

Back 32

Low concentration: D1 receptors --> vasodilation; increased GFP, RBF, Na excretion
High concentration: increased inotropy (B1); increased systolic BP; vasoconstriction (a1)

Hint 32

Shock

Front 33

Fenoldopam

Back 33

D1-receptor agonist

Hint 33

In-hospital, short-term management of severe HTN
Continuous IV infusion

Front 34

Isoproterenol

Back 34

B1 & 2 agonist

Absorbed by sublingual mucosa; better absorbed parenterally or inhaled
Stable to MAO

Hint 34

Stimulate heart in emergency situations

Front 35

Dobutamine

Back 35

Racemic mixture --> B1 agonist

Hint 35

Increase CO in acute heart failure --> little change in HR and oxygen demand

Adverse: use in caution with atrial fib

Front 36

Terbutaline

Back 36

B2 agonist

Hint 36

Bronchodilator and reduce uterine contractions in premature labor
Parenterally for emergency treatment of status asthmaticus

Front 37

Albuterol (salbutamol)

Back 37

B2 agonist

Hint 37

Inhalant to relieve bronchospasm

Front 38

Salmeterol

Back 38

B2 agonist

Prolonged duration of action: 12 hrs; slow onset of action

Hint 38

Not suitable alone for prompt relief of bronchospasm

Front 39

Formoterol

Back 39

B2 agonist

Long-acting; similar to salmeterol

Front 40

Phenylephrine

Back 40

A1 agonist

Vasoconstrictor: raises systolic and diastolic BP

Given parenterally, induces reflex bradycardia

Hint 40

Used as nasal decongestant & as mydriatic
Used to increase BP & terminate supraventricular tachycardia

Large doses can cause HTN headaches and cardiac irregularities

Front 41

Clonidine

Back 41

Partial A2 agonist

Centrally acting anti-HTN (suppresses sympathetic outflow from brain)

Hint 41

IV infusion causes transient increase in BP --> not seen if given orally

Front 42

Methyldopa

Back 42

A2 agonist

Centrally acting anti-HTN

Hint 42

Drug of choice for treatment of HTN during pregnancy

Adverse: sedation, mental lassitude; impaired concentration

Front 43

Brimonidine

Back 43

A2 agonist

Hint 43

Lowers intraocular pressure in glaucoma --> reduces aq humor production and increases uveoscleral outflow

Front 44

Amphetamine

Back 44

Displaces endogenous catecholamines from vesicles
Weak MAOI
Blocks reuptake

Hint 44

See notes

Front 45

Methylphenidate

Back 45

Analog to amphetamine

Hint 45

ADHD

Front 46

Tyramine

Back 46

Normal by-product of tyrosine metabolism
Oxidized by MAO

Hint 46

If patient taking MAOI, can cause serious vasopressor episodes

Front 47

Ephedrine

Back 47

Mixed action agonist
A & B receptors and releases NE
Long action duration
Oral absorption and penetrates CNS

Hint 47

Asthma
Nasal decongestant
Raise BP

Front 48

Oxymetazoline
Xylomethazoline

Back 48

A agonist

Hint 48

Decrease nasal mucosa volume by activating A1 receptors

Front 49

Phenylephrine
Pseudoephedrine

Back 49

Agonist

Hint 49

Oral preparation for nasal congestion relief
Found in combination with H1-histamine antagonist

Front 50

Phenoxybenzamine

Back 50

Irreversibly blocks A receptors

Prevents vasoconstriction of peripheral BV --> reflex tachycardia

Hint 50

Treats pheochromocytoma
Beta blocker may be given after to control tachycardia --> beta blocker should NEVER be given before A blockade due to increased vasoconstriction
Adverse:
Postural hypotension, nasal stuffiness, N & V
Inhibit ejaculation
May induce tachycardia

Front 51

Phentolamine

Back 51

Reversibly blocks A1 & 2
Reflex cardiac stimulation & tachycardia via baroreceptor & blocking A2 receptors of cardiac symp nerves

Hint 51

Prevention or control of HTN episodes
Diagnosis of pheochromocytoma
Prevention of dermal necrosis
HTN crisis of drug overdose
HTN crisis of sudden withdrawal of anti-HTN drugs (e.g. clonidine)
HTN crisis from interaction of MAOI and tyramine

Front 52

Prazosin

Back 52

A1 selective blocker
Decreases peripheral resistance and relaxes both arterial and venous SM --> no reflex tachycardia
CNS to suppress sympathetic outflow
Decreases LDL & TAGs, increases HDL

Hint 52

Approved for HTN

Front 53

Terazosin
Doxazosin

Back 53

Analogs of prazosin

Hint 53

HTN & BPH

Front 54

Tamsulosin

Back 54

A1 blocker - A1A blocker --> receptor dominates at genitourinary SM

Hint 54

BPH
Little effect on BP

Front 55

Yohimbine

Back 55

A2 blocker --> leads to release of NE --> stimulates B1 & A1
Also causes insulin release

Hint 55

Can abruptly reverse anti-HTN effects of A2 agonist --> contraindicated

Front 56

Propranolol

Back 56

Beta blocker

Reduction in CO, renin release, in central sympathetic activity

Contraindicated in patients with asthma

Hint 56

HTN
Glaucoma
Migraine
Hyperthyroidism
Angina pectoris --> contraindicated in variant angina
Atrial fibrillation
MI --> prophylactic for 2nd MI, reduces infarct size and speeds recovery
Performance anxiety
Adverse:
Bronchoconstriction; arrhythmias; diabetics & elevate TAGs and decrease HDL

Front 57

Nadolol

Back 57

Beta blocker

Longer action duration

Hint 57

Long-term management of patients with angina pectoris
HTN

Front 58

Timolol

Back 58

Beta blocker

Hint 58

HTN
Prophylaxis for migraines
Intraocular HTN or open-angle glaucoma

Front 59

B1 antagonists

Back 59

Atenolol, metoprolol, esmolol

Hint 59

Decrease BP in HTN
Increase exercise tolerance in angina
HTN patient with impaired pulmonary fxn
Diabetic HTN pts receiving insulin

Front 60

Esmolol

Back 60

B1 antagonist
Ultra short acting

Hint 60

Given IV
Used when beta blockade is desired

Front 61

Propranolol

Back 61

Beta blocker

Reduction in CO, renin release, in central sympathetic activity

Contraindicated in patients with asthma

Hint 61

HTN
Glaucoma
Migraine
Hyperthyroidism
Angina pectoris --> contraindicated in variant angina
Atrial fibrillation
MI --> prophylactic for 2nd MI, reduces infarct size and speeds recovery
Performance anxiety
Adverse:
Bronchoconstriction; arrhythmias; diabetics & elevate TAGs and decrease HDL

Front 62

Nadolol

Back 62

Beta blocker

Longer action duration

Hint 62

Long-term management of patients with angina pectoris
HTN

Front 63

Timolol

Back 63

Beta blocker

Hint 63

HTN
Prophylaxis for migraines
Intraocular HTN or open-angle glaucoma

Front 64

B1 antagonists

Back 64

Atenolol, metoprolol, esmolol

Hint 64

Decrease BP in HTN
Increase exercise tolerance in angina
HTN patient with impaired pulmonary fxn
Diabetic HTN pts receiving insulin

Front 65

Esmolol

Back 65

B1 antagonist
Ultra short acting

Hint 65

Given IV
Used when beta blockade is desired

Front 66

Labetalol

Back 66

Competitive antagonist at B & A1

Hint 66

HTN of pheochromocytoma and HTN emergencies
Adverse:
Orthostatic hypotension & dizziness (A1 blockade)

Front 67

Carvedilol

Back 67

B antagonist & A1 antagonist

Antioxidant properties

Hint 67

HTN & CHF

Front 68

Pindolol

Back 68

Beta partial agonist --> possesses ISA

Hint 68

HTN management

Front 69

Cocaine

Back 69

Blocks uptake of monoamines --> blocks DAT, SERT, NET

Hint 69

In CNS, blocks dopamine reuptake in limbic system
Blocks voltage-gated sodium channels

Front 70

Methyltyrosine (metyrosine)

Back 70

Competitive inhibitor of tyrosine hydroxylase --> interferes with dopamine synthesis

Hint 70

Used with phenoxybenzamine & other A blockers for pheochromocytoma

Front 71

Reserpine

Back 71

Irreversibly damages VMAT
--> vesicles can't store & concentrate NE & dopamine --> depletion of NE

Hint 71

HTN --> gradual decrease in BP & HR
Slow action onset; long action duration

Front 72

Guanethidine

Back 72

Displaces NE from vesicles & inhibits release from nerve endings (affects AP triggering)

Parasympathetics not altered

Hint 72

Gradual decrease in BP & HR
Causes orthostatic hypotension