Autonomic Drug

Question 1

Onabotulinum toxinA

Answer 1

In activates synaptic vesicles protein (SNAP-25), prevents docking with membrane and therefore no ACh release; flaccid paralysis of skeletal muscles; indications: muscle spasms, cosmetic, auxiliary hyperhidrosis, overactive bladder

Question 2

Onabotulitum toxin S.E

Answer 2

Distant spread beyond injection site; dysphasia and breathing difficulties, ptosis, pain, drooling, loss of facial expression

Question 3

Muscarine

Answer 3

Selectively stimulates M1-M5

Question 4

Atropine

Answer 4

Selectively blocks M1-M5

Question 5

Nicotine

Answer 5

Stimulates Nn and Nm, blocked by mecamylamine

Question 6

D-tubocurarine

Answer 6

Competitive antagonist of Nm

Question 7

Reserpine

Answer 7

Inhibits the storage of catecholamines therefore increases degradation by MAO, depleting nerve terminals and reducing SNS in CNS and periphery; oral anti-HTN and antipsychotic

Question 8

Tyramine

Answer 8

Stimulation of NE release- displaces NE from vesicles and causes non-vesicular release; can elicit a HTN crisis

Question 9

Methyldopa

Answer 9

Prodrug converted to methyl-NE and is a selective alpha-2 agonist, decreasing SNS outflow to periphery; SE=sedation, dry mouth, Parkinsonism, hyperprolactinemia

Question 10

Cocaine

Answer 10

Inhibition of catecholamines termination, blocks NET allowing for excess SNS stimulation

Question 11

Acetylcholine

Answer 11

Non-selective action at M and Nn; IV, short duration

Question 12

Bethanechol

Answer 12

Prototype ester; selective M agonist, postoperative and postpartum urinary retention, GERD, gastric atony; resistant to hydrolysis by cholinesterase

Question 13

Pilocarpine

Answer 13

Partial agonist of all muscarinic receptor subtypes; prototype alkaloid; used typically in eyes to produce mitosis and blurred vision, decrease in IOP (xerostomia and wide-angle glaucoma are indications)

Question 14

Cevimeline

Answer 14

Selective M3 agonist; used to treat dry mouth

Question 15

Anticholinergic side effects

Answer 15

“Hot as a hare, dry as a bone, blind as a bat, red as a beet, mad as a hatter”

Question 16

Scopolamine

Answer 16

Muscrarinic antagonist; CNS penetration better than atropine; sedation at low doses; suppresses eyes is and motion sickness by blocking M in vestibular system

Question 17

Ipatropium bromide

Answer 17

Muscarinic antagonist that does not cross membranes, stays locally; used as an inhaled broncodilator for treatment of asthma and COPD

Question 18

Tropicamide

Answer 18

Muscarinic antagonist; mydriatic and cycloplegic; facilitates diagnosis and surgery of eyes, short length of duration (6 hours)

Question 19

Tolterodine

Answer 19

Non-selective muscarinic antagonist; used in the treatment of overactive bladder

Question 20

Neostigmine

Answer 20

Anti cholinesterase agent also an agonist at the NMJ; tx for myasthenia gravis to increase ACh levels at NMJ

Question 21

Physostigmine

Answer 21

AChE inhibitor; crosses BBB; used to treat poisoning by atropine

Question 22

Donepezil

Answer 22

More selective inhibition of AChE isoform in the CNS; used to tx cognitive decline in Alzheimer’s

Question 23

Malathion

Answer 23

Irreversible inhibitor of AChE

Question 24

Tx for malathion poisoning

Answer 24

Atropine or Pralidoxime (AChE reactivator)

Question 25

Epinephrine

Answer 25

(Alpha-1, alpha-2, beta-1, beta-2)

Adrenergic agonist

Question 26

Norepinephrine

Answer 26

(Alpha-1, alpha-2, beta-1)

TX: Severe hypotensive states, vasopressin for treatment of septic shock

Question 27

Isoproterenol

Answer 27

(Beta-1, beta-2)
Potent, non-selective beta agonist
Tx: AV block and cardiac arrest, broncospasm during anestheisa

Question 28

Dopamine

Answer 28

(D1 > beta-1 > alpha-1)
Adrenergic agonist
Tx: treatment of shock if accompanied by low cardiac output, maintain systemic blood pressure in hypotensive patients

Question 29

Dobutamine

Answer 29

(Beta-1)
Adrenergic agonist
Increases contractility and heart rate
Tx: short term management of severe refractory CHF

Question 30

Phenylephrine

Answer 30

(Alpha 1)
Non-catecholamine adrenergic agonist
Tx: nasal decongestant, vasopressin agent, mydriatic, detumescent

Question 31

Clonidine

Answer 31

(Alpha-2)
Non-catecholamine adrenergic agonist
Tx: hypertension, relief of severe pain

Question 32

Terbutaline

Answer 32

(Beta-2)
Non-catecholamine adrenergic agonist
Tx: reduces airway resistance in asthmatics with little effect on heart

Question 33

Tamsulosin

Answer 33

Adrenergic antagonist (alpha-1a)
Selectively favors blockade in prostate capsule, urethra and bladder neck with little effect on BP

Question 34

Prazosin

Answer 34

Alpha Adrenergic antagonist (alpha-1)
Dilates arteries and veins and relaxes smooth muscle of the bladder neck and prostate capsule
Tx: third line agent for hypertension

Question 35

Propranolol

Answer 35

Beta Adrenergic antagonists (Beta-1, beta-2)

Pure competitive antagonist: decrease HR and slow impulse conduction through AV node, long term reduces blood pressure

Question 36

Metoprolol

Answer 36

Beta Adrenergic antagonist; 2nd generation “cardio selective”; highly selective for beta-1 receptors at therapeutic doses, less likely to causes bronchoconstriction and suppression of glycogenolysis
Tx: HTN, angina, CHF, MI

Question 37

Mecamylamine

Answer 37

N(n) antagonist, noncompetative, blocks activation of SNS and PNS nerve fibers, reveals dominant division affecting the tissue; anti-HTN agent