Drugs Block 1

Question 1

Propanolol

Answer 1

a nonselective beta-adrenergic receptor antagonist; used to tx hypertension, migraines, tremors, and arrhythmia.

Question 2

Albuterol

Answer 2

a selective β2-adrenergic receptor agonist; bronchodilator used oto tx asthma; receptor activation works to activate downstream adenylate cyclase -→ increase in cAMP which promotes smooth muscle relaxation.

Question 3

Acetaminophen

Answer 3

NSAID class; antipyretic and analgesic; noncompetitive antagonist (inhibitor) for arachidonic acid at COX1 and COX2; prevents prostaglandin synthesis

Question 4

Ibuprofen

Answer 4

NSAID class; antipyretic, analgesic and anti-inflammatory; competitive antagonist (inhibitor) for arachidonic acid at COX1 and COX2; prevents prostaglandin synthesis

Question 5

Ketoprofen

Answer 5

NSAID class; antipyretic, analgesic and anti-inflammatory; competitive antagonist (inhibitor) for arachidonic acid at COX1 and COX2; prevents prostaglandin synthesis; more potent than Ibuprofen

Question 6

Phenobarbital

Answer 6

a barbiturate; agonist at GABA channel; GABA normally activates Cl- channel, leading to membrane hyperpolarization, and reduced excitability of post-synpatic cell; has anticonvulsant (anti-epileptic) and sedative properties; increases probability of Cl- ch. being open; also directly activates the channel in absence of GABA.

Question 7

Diazepam

Answer 7

a benzodiazepine; agonist at GABA channel; GABA normally activates Cl- channel, leading to membrane hyperpolarization; reduces excitability of post-synpatic cell; has anticonvulsant and sedative properties; used to tx EtOH withdrawal, anxiety, seizure, spasms, aslo used as sedative for procedures; increases probability of Cl- ch. being open

Question 8

Gamma hydroxybutyrate

Answer 8

in salt form called sodium oxybate; a CNS depressant used therapeutically to treat narcolepsy and EtOH withdrawal, but also widely abused due to euphoric effects; modulates K+ and Ca+2 channels via GPCR receptors (GABAB and GHB receptor); has a short half-life and low therapeutic index; horrible withdrawal effects (tremor, tachycardia, restlessness, insomnia, anxiety, N/V, delirium, diaphoresis, HTN, coma, and death). Can given pt’s Baclofen (GABAB agonist) to help decrease withdrawal sxs.

Question 9

Diltiazem

Answer 9

a L-type calcium channel antagonist; used to treat high BP, SVT, angina, vasospasm w/ SAH, and premature labor; reduced Ca entry→smooth muscle relaxation

Question 10

Nifedipine

Answer 10

a dihydropyridine; L-type calcium channel antagonist; leads to relaxation of vascular smooth muscle; used as antihypertensive

Question 11

Verapamil

Answer 11

a L-type calcium channel antagonist; used to treat high BP, SVT, angina, vasospasm w/ SAH, and premature labor; reduced Ca entry → smooth muscle relaxation

Question 12

Erythromycin

Answer 12

antibiotic; also HERG channel antagonist ( K+ ch that repolarizes Vm); leads to prolonged ventricular depolarization and delayed repolarization—Long QT syndrome (predisposition to ventricular arrhythmias)

Question 13

Sildenafil

Answer 13

inhibits cGMP specific phosphodiesterase Type 5 (PDE5) in smooth muscle; prevents breakdown of cGMP → GMP, thereby preventing muscle relaxation; used to tx erectile dysfunction and pulmonary hypertension;

Question 14

Minoxidil

Answer 14

K+ channel agonist; influx of K+ will hyperpolarize the membrane potential thus preventing ctxn and promoting relaxation of vascular smooth muscle; used as an antihypertensive and to treat male/female pattern hair loss.

Question 15

Diazoxide

Answer 15

K+ channel agonist; blocks insulin release from pancreas, also has extrapancreatic (catecholamine-induced) effect used to treat hypoglycemia (due to hyperinsulinemia); also an arteriole vasodilator used to tx malignant HTN

Question 16

Glibenclamide

Answer 16

a sulfonylurea; antagonist for KATP channels; leads to depolarization of islet cells and subsequent release of insulin; used to tx Type 2 DM.

Question 17

Glipizide

Answer 17

a sulfonylurea; antagonist for KATP channels; leads to depolarization of islet cells and subsequent release of insulin; used to tx Type 2 DM.

Question 18

Tolbutamide

Answer 18

a sulfonylurea; direct antagonist for KATP channels in absence of ATP; leads to depolarization of islet cells and subsequent release of insulin; used to tx Type 2 DM.

Question 19

Octreotide

Answer 19

a naturally occurring somatostatin analogue; decreases endocrine-secretions; can be used to reduce insulin secretion to treat hyperinsulinemia.

Question 20

Procaine

Answer 20

aka Novocaine; local anesthetic; gold standard for 50 years; slow onset/short lived (ester linkage); lasts 0.5-1 hr; has maximum dose 3-4X higher than other LA’s. Administered via spinal, infiltration, peripheral nerve block

Question 21

Tetracaine

Answer 21

aka Pontocaine; local anesthetic used for eye surgery; ester linkage, more lipophilic; duration 1.5-6 hours (relatively long); administered via spinal or topical

Question 22

Benzacaine

Answer 22

aka Hurricane; local anesthetic used in anesthetizing surfaces (topical route); major component of Cetacaine topical spray; not water soluble, no tertiary amine—acts only as un-ionized drug; duration 0.5-1 hr; 20% conc. (very high)

Question 23

Cocaine

Answer 23

local anesthetic, clinically useful, but abuse liability and cardiotoxicity; ester linkage (slower onset, short-lived), duration 0.5-1 hr; administered topically

Albert Niemann, German chemist first to isolate cocaine. William Halsted, American surgeon who popularized used of cocaine in anesthesia, also an addict.

Question 24

Lidocaine

Answer 24

aka Xylocaine; a Na+ channel antagonist, used as local anesthetic for dermatological lacerations (also intubations); 30% in un-ionized form; amide linkage (faster onset, longer lasting); duration 0.75-2 hrs; used to block nerve conduction or lower concentration to treat VT in ischemic heart. Administered in all routes (except orally).

Question 25

Bupivacaine

Answer 25

aka Marcaine; local anesthetic used in obstetrics as epidural; also for local infiltration, peripheral nerve block, IV regional, and topical; has amide linkage (fast onset, long lasting), duration 0.5-8 hours; hydrolyzed by esterases and amidases; most lipophilic (more potent)

Question 26

Nicotine

Answer 26

agonist of nicotinic receptor in ganglia; affects CV system by elevating BP and HR; also affects CNS (EEG arousal to decreased muscle tone, convulsions).

Question 27

Succinylcholine

Answer 27

nAChr agonist that causes transient depolarization, followed by desensitization of ACh channels; keeps EPP depolarized as long as it is bound to nAChr (and not broken down by AChE, so long-lasting) thereby inactivating surrounding sodium channels, which cannot recover till EPP repolarizes. Used as a depolarizing block, often in emergent intubating due to fast onset of paralysis.

Question 28

Varenicline

Answer 28

aka Chantix; partial agonist of nAChR; primary effects are CNS, used for smoking cessation.

Question 29

Rocuronium

Answer 29

competitive antagonist of nicotinic-ACh receptor; used to produce non-depolarizing block (muscle paralysis) during surgery

Question 30

Cisatracurium

Answer 30

a competitive antagonist of nicotinic-ACh receptor; used to produce non-depolarizing block (muscle paralysis) during surgery; metabolized differently than rocuronium.

Question 31

Trimethaphan

Answer 31

a short acting antagonist of ganglionic nicotinic receptors; blocks transmission in parasympathetic and sympathetic ganglia; used for hypertensive emergencies and autonomic testing.

Question 32

Edrophonium

Answer 32

aka Tensilon; anticholinesterase used to improve eye muscle strength/control in MG patients; also used to dx MG.

Question 33

Neostigmine

Answer 33

anticholinesterase used to tx MG and to reverse neuromuscular blocks; binds to AChE via esteratic and anionic sites

Question 34

Pyridostigmine

Answer 34

prophylactic tx for anticholinesterase nerve agents; used by soldiers in areas with high risk of chemical weapons attacks. Also used commonly for maintenance in myasthenia gravis.

Question 35

Sarin

Answer 35

typical organophosphate anticholinesterase, binds esteratic site via PO43-

Question 36

Malathione

Answer 36

thiophosphate insecticide, used in humans to tx head lice; generally safe because even though malathion (inactive form) gets converted to malaoxon (active form) by desulfuration, malaoxon is hydrolyzed (inactivated) even more quickly, so there is no build up of active product.

Question 37

Atropine

Answer 37

PRIMARY tx for anticholinersterase nerve agents

Question 38

Acetylcholine

Answer 38

agonist of nicotinic acetylcholine receptors; NT for skeletal muscle motor efferents

Question 39

Pralidoxime

Answer 39

2nd line treatment for organophosphate toxicity

Question 40

Tetrodotoxin

Answer 40

aka TTX; voltage-gated Na+ channel inhibitor

Question 41

Botulium toxin

Answer 41

aka Botox; blocks Ca2+ mediated exocytosis of ACh into synaptic cleft; FDA approved to tx muscle spasms

Question 42

Tetraethylammonium

Answer 42

aka TEA; inhibits voltage-gated K+ channels