Exam 3 - ANS drugs Flashcards

1
Q

Epinephrine

A

non-selective agonist; used for cardiac emergencies, allergic response, local anesthetics; increase BP (B1, a1), bronchiole dilation (B2), glycogenolysis/gluconeogenesis (B2)

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2
Q

norepinephrine

A

a1, a2, B1 agonist; use for cardiac emergencies but effect can be variable -> bradycardia, local anesthetics

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3
Q

dopamine

A

a1, B1 agonist; can be used for cardiac emergencies, cause vasodilation in the renal arteries

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4
Q

dobutamine

A

a1, B1, B2 agonist; 2 isomers whose net effect is a B1 agonist -> increase heart contractile force

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5
Q

Catcholamine metabolism

A

rapidly broken down in GI tract and liver (lots of MAO); ineffective with oral administration

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6
Q

phenylephrine

A

a1 agonist; used as nasal decongestant, for blood shot eyes, and in hypotensive emergencies

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7
Q

clonidine

A

a2 agonist; a2 activation in CNS lowers sympathetic tone, treats chronic hypertension suppresses withdrawal symptoms in opioid addicts, irritant in eye

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8
Q

brimonidine

A

a2 agonist; main treatment of glaucoma by decreasing synthesis of aqueous humor, decreasing intraocular pressure

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9
Q

isoproterenol

A

B1, B2 agonist; treats asthma, but can activate B1 receptors

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10
Q

albuterol

A

B2 agonist; treats asthma

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11
Q

terbutaline

A

B2 agonist; activated in the uterus to suppress uterine contractions in premature labor

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12
Q

amphetamine

A

indirect adrenergic agonist, releaser; treats ADHD, narcolepsy, chronic fatigue syndrome; causes vesicle transporter to pump norepinephrine into the varicosity and then uptake transport pumps it into the effector cell junction -> activate adrenergic receptors

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13
Q

methylphenidate

A

indirect adrenergic agonist, releaser; treats ADHD, affects CNS, less peripheral (cardiovascular) effects than amphetamine

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14
Q

Tyramine

A

indirect adrenergic agonist, releaser; acts as neurotransmitter, avoid intake when using MAO inhibitors

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15
Q

Cocaine

A

indirect adrenergic agonist, uptake inhibitor; local anesthetic, CNS effects; blocks neuronal uptake transporter (re-uptake)

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16
Q

Tricyclic antidepressants

A

indirect adrenergic agonist, uptake inhibitor

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17
Q

Inhibitors of metabolism (MAO inhibitors)

A

indirect adrenergic agonist, blocks breakdown of catecholamines

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18
Q

Ephedrine

A

a, B mixed adrenergic agonist; ephinephrine and amphetamine-like activity; use for incontinence (loss of bladder control)

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19
Q

phentolamine

A

a1, a2 antagonist; use for acute hypertension, but heart rate increases

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20
Q

prazosine

A

a1 antagonist; use for chronic hypertension; 1st dose effect, epinephrine reversal

21
Q

tamsulosin

A

a1A antagonist; use to treat prostate hyperplasia -> relaxes smooth muscle, pressure on urethra -> improve urination

22
Q

propranolol

A

B1, B2 antagonist; use for lowering BP, vasodilation even though _2 blocked; contraindicated in asthmatics and T1D patients

23
Q

timolol

A

B1, B2 antagonist; treats glaucoma, reduces aqueous humor synthesis; contraindicated in asthmatics and T1D patients

24
Q

metoprolol

A

B1 antagonist; lowers BP, can be used in asthmatics and T1D patients

25
Q

labetalol

A

a1 antagonist, B receptor partial agonist; 3rd generation B blocker, lowers BP

26
Q

Reserpine

A

indirect antagonist; lowers BP (less binding to a1, B1) irreversibly binds to VMAT so norepinephrine can not enter vesicles and instead broken down by MAO; can enter CNS -> parkinsonism

27
Q

Botulinum toxin

A

in cholerginic fibers, prevent fusion of storage vesicles to the membrane -> treat cerebral palsy, particular spastic muscles

28
Q

Black widow spider venom

A

in cholerginic fibers, causes massive fusion of storage vesicles to the membrane

29
Q

Acetylcholine

A

cholinergic agonists, choline esters; rapidly hydrolysed by cholinesterases

30
Q

Carbachol

A

cholinergic agonists, choline esters; has muscarinic and nicotinic activity; only used as eye drops to treat glaucoma

31
Q

Bethanechol

A

cholinergic agonists, choline esters; has only muscarinic activity; treats paralytic ileus and bladder atony

32
Q

Pilocarpine

A

cholinergic agonists, alkaloids; has only muscarinic activity; treats xerostomia (saliva production is reduced) and glaucoma

33
Q

Adverse effects of muscarinic agonists

A

SLUD (salivation, lacrimation, urination, defecation); bronchiolar smooth muscle contraction

34
Q

Donepezil

A

Rapidly reversible non-covalent cholinesterase inhibitors; treats Alzheimer’s disease

35
Q

Physostigmine

A

Rapidly reversible covalent carbamate cholinesterase inhibitors; treats glaucoma, only used topically

36
Q

Neostigmine

A

Rapidly reversible covalent carbamate cholinesterase inhibitors; treats glaucoma (systemically), co-administered with bethanechol, treat myasthenia gravis

37
Q

Carbaryl

A

Rapidly reversible covalent carbamate cholinesterase inhibitors; used in pesticides, can cause cholinergic crises (SLUD)

38
Q

Echothiophate

A

Slowly reversible organophosphate cholinesterase inhibitors; treats glaucoma (topically), 1 drop every 4 days

39
Q

Parathion

A

Slowly reversible organophosphate cholinesterase inhibitors; used as an agricultural pesticide

40
Q

Soman

A

Slowly reversible organophosphate cholinesterase inhibitors; nerve gas -> very potent, volatile, lipid soluble, aging occurs instantly

41
Q

2-PAM

A

antidote that is better at removing phosphate on serine hydroxyl of cholinesterase than water, but can not stop aging; can not be used for carbamate toxicity since it makes it worse

42
Q

Atropine

A

natural alkaloid muscarinic blocker; many indications -> opposite effects of parasymathetic response but can cause increased body temperature and dry mouth

43
Q

Scopolamine

A

natural alkaloid muscarinic blocker; anti-nausea

44
Q

Ipratropium

A

synthetic quaternary amine muscarinic blocker; treats asthma

45
Q

Benztropine

A

synthetic tertiary amine muscarinic blocker; reduces severity of early state Parkinson’s disease

46
Q

Mecamylamine

A

ganglionic blocker; acts in ANS to treat hypertension; side effect - orthostatic hypotension

47
Q

How to treat organophosphate intoxication?

A

2-PAM and atropine

48
Q

How to treat carbamate intoxication ?

A

Atropine