Summary of Drug Actions Flashcards

1
Q

Donepezil

A

Inhibition of acetylcholine degradation, acetylcholinesterase, Alzheimers

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2
Q

Rivastigmine

A

inhibition of acetylcholine degradation, acetylcholinesterase, Alzheimers

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3
Q

Edrophonium

A

Inhibition of acetylcholine degradation, acetylcholinesterase, Edrophonium test

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4
Q

Pyridostigmine

A

inhibition of acetylcholine degradation, acetylcholinesterase, Myasthenic Syndrome (LEMS)

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5
Q

Echothiophate

A

inhibition of acetylcholine degradation, acetylcholinesterase, Glaucoma

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6
Q

What is the rate limiting step of acetylcholine biosynthesis?

A

choline uptake into presynaptic neuron by Na dependent choline transporter (CHT)

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7
Q

Hemicholinium

A

highly toxic, can inhibit choline transporter.

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8
Q

What is acetylcholine (made) synthesized from?

A

AcCoA and choline by ChAT (choline acetyltransferase)

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9
Q

Organomercury

A

inhibitor of choline acetyltransferase (ChAT)

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10
Q

Vesicle acetylcholine transporter (VAT) coupled with proton efflux

A

storage. acetylcholine is being uptake.

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11
Q

what happens when Ca2+ channels are attacked by autoantibodies (after release)

A

Lambert Eaton Myasthenia Syndrome (LEMS)

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12
Q

Vesamicol

A

inhibitor of acetylcholine UPTAKE

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13
Q

Botulinum toxin

A

fusion process of acetylcholine inhibited by this.

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14
Q

CHT (choline transporter)

A

choline can be reuptake back into the presynaptic neuron and used for regular uptake into presynaptic neuron too.

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15
Q

What diseases are associated with acetylcholine?

A

Alzheimers
Lambert-Eaton Myasthenia Syndrome
Glaucoma

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16
Q

What effect does excess acetylcholine have on memory and learning?

A

none.

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17
Q

What effect does not enough acetylcholine have on memory and learning

A

alzheimers

18
Q

What is LEMS caused by

A

not enough acetylcholine, less movement

19
Q

What is Glaucoma and Esotropia caused by?

A

Not enough acetylcholine, less fluid from the eye.

20
Q

What does acetylcholine bind to on the postsynaptic membrane?

A

cholinergic: nicotinic (ionotropic) or muscarine (metabotropic) receptors

21
Q

Fast synaptic transmission, Excitatory, found in the brain, autonomic ganglia, adrenal medulla, and neuromuscular junction.

A

nicotinic receptors (ionotropic)

22
Q

Slow metabolic response, excitatory or inhibitory. found in brain, heart, and smooth muscles.

A

Muscarinic receptors (metabotropic)

23
Q

What is the signal transduction of nicotinic receptors?

A

form pores through the cell membrane
control influx of Na+, K+, or Ca2+ at synapses.
trigger membrane depolarization
mediate fast transmission of nerve impulses

24
Q

Which receptor needs two binding site to be occupied to activate the receptors?

A

nicotinic.

25
Q

Nicotine

A

agonist, Nn receptor, smoking cessation (nicotinic)

26
Q

Cytisine

A

in brain, agonist, Nn receptor, smoking cessation (nicotinic)

27
Q

Varenicline

A

in brain, agonist, Nn receptor, smoking cessation (nicotinic)

28
Q

Succinylcholine

A

agonist, Nm receptors, Anesthesia. (nicotinic)

29
Q

Hexamethonium

A

antagonist, Nn receptor, hypertension (nicotinic)

30
Q

Rocuronium

A

Antagonist, Nm receptors, Anesthesia Paralysis. (nicotinic receptor)

31
Q

Xanomeline

A

selective for M1, M4 only (muscarinic)

32
Q

Pilocarpine

A

selective for M3. Glaucoma, Dry mouth, Cystic Fibrosis (muscarinic)

33
Q

Bethanechol

A

Agonist, m1-m5, urinary retention (muscarinic)

34
Q

Carbachol

A

agonist, m1-m5 nm&nn. glaucoma and urinary retention. (muscarinic)

35
Q

Methacholine

A

agonist, m1-m5, bronchial challenge test. (muscarinic)

36
Q

Eye: iris circular muscle
ciliary muscle

A

agonist: contracts, antagonist does the opposite. Mydriatic (muscarinic)

37
Q

Heart:
Sinoatrial node
Atrial contractility

A

agonist: decelerates, antagonist does the opposite. Bradycardia. (muscarinic)

38
Q

Lung: Smooth muscle

A

Agonist: contracts, antagonist does the opposite. Asthma and allergic rhinitis. (muscarinic)

39
Q

Bladder: Smooth muscle

A

Agonist: contracts, antagonist does the opposite. overactive bladder. (muscarinic)

40
Q

Gastrointestinal tract : Smooth muscle (there are more for GI)

A

Agonist: contracts, antagonist does the opposite. GI antispasmodic (muscarinic)

41
Q

GI: Secretions

A

Agonist: Increases. Antagonist does the opposite. GI antispasmodic (muscarinic)

42
Q

GI: sphincters

A

Agonist: relaxes. Antagonist does the opposite. GI antispasmodic. (muscarinic)