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PHCOL 402 > Drugs (Midterm I) > Flashcards

Drugs (Midterm I) Flashcards

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1
Q

Nicotine, DMPP, TEA

A

Class: Nicotinic Ganglionic Stimulating Receptors
MOA: Activate and desensitize nAChR in ganglionic synapses

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2
Q

Muscarine, Pilocarpine

A

Class: Muscarinic Ganglionic Stimulating Drugs
MOA: Stimulate mAChR and stimulates sympathetic nervous system via late EPSP

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3
Q

Pentolinium, TEA, Hexamethanonium

A

Class: Ganglionic Blockers
MOA: competitive antagonists and block nAChR

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4
Q

Botulinum Toxin

A

MOA: Inhibits ACh by entering the nerve terminal and acts as a protease to prevent neurotransmitter release

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5
Q

Gallamine, Curarine, Pancurenium

A

Class: Neuromuscular Blockers (Competitive non-depolarizing blocker)
MOA: Classical competitive antagonists at the nAChRs

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6
Q

Decamethonium-C10, Succinyl Choline

A

Class: Neuromuscular Blockers (Depolarizing blocker)
MOA: Partial agonists that bind to the receptors and activate them but antagonize ACh action

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7
Q

Edrophonium (a), neostigmine (b), DFP (c), echothiophate (c)

A

Class: Acetylcholinesterase blockers
MOA: Prevents the breakdown of ACh, increasing ACh in the synapse

There are 3 types: a) Reversible, b) Carbamate esters, c) Organophosphates

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8
Q

Activate and desensitize nAChR in ganglionic synapses

A

Nicotinic Ganglionic Stimulating Receptors (Nicotine, DMPP, TEA)

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9
Q

Stimulate mAChR and stimulates sympathetic nervous system via late EPSP

A

Muscarinic Ganglionic Stimulating Drugs (Muscarine, Pilocarpine)

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10
Q

Competitive antagonists and block nAChR

A

Ganglionic Blockers (Pentolinium, TEA, Hexamethanonium)

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11
Q

Inhibits ACh by entering the nerve terminal and acts as a protease to prevent neurotransmitter release

A

Botulinum Toxin

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12
Q

Classical competitive antagonists at the nAChRs

A

Neuromuscular Blockers (Competitive non-depolarizing blocker: Gallamine, Curarine, Pancurenium)

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13
Q

Partial agonists that bind to the receptors and activate them but antagonize ACh action

A

Neuromuscular Blockers (Depolarizing blocker: Decamethonium-C10, Succinyl Choline)

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14
Q

Prevents the breakdown of ACh, increasing ACh in the synapse

A

Acetylcholinesterase blockers

There are 3 types: a) Reversible: Edrophonium, b) Carbamate esters: neostigmine, c) Organophosphates: echothiophate, DFP

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15
Q

Carbachol, Bethanechol, Bethanecholamine, ACh

A

Class: Choline esters
MOA: mAChR and nAChR agonists (except bethanechol, not an agonist at nAChR)

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16
Q

Muscarine, Arecoline, Pilocarpine, Oxotremorine, Aceclidine

A

Class: Cholinomimetic Alkaloids
MOA: Mimics choline esters, relatively selective for mAChRs except arecoline which also activates nAChRs.

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17
Q

Belladonna

A

Class: Antimuscarinic drugs
MOA: Reversible inhibition of mAChRs, block parasympathetic stimulation

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18
Q

N-methylatropine, Ipratropium, Scopolamine

A

Class: Quaternary Muscarinic Antagonists
MOA: Antagonists to the mAChR and the nAChR

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19
Q

Atropine, Diphenhydramine (Benadryl), tricyclics, Scopolamine (anti mAChRs)
Curare, Hexamethonium (anti nAChRs)

A

Class: Anticholinergics
MOA: Competitively inhibit binding of ACh, more commonly in mAChRs, less so in nAChRs

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20
Q

Physostigmine, Neostigmine

A

Class: Anticholinesterases
MOA: Cholinometric effects at both nicotinic and muscarinic synapses by inhibiting AChE

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21
Q

Albuterol, Ritodrine, Tertbutaline, Salmeterol

A

Class: b2AR agonists
MOA: Mostly selective for b2ARs, will stimulate cAMP and PKA. Relaxation of VSM, bronchodilators, can delay labor (ritodrine), some have cardio effects

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22
Q

Dobutamine

A

One isomer is an a1 agonist, the other an a1 antagonist. b1AR antagonist, increases heart rate

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23
Q

Fenoldopam

A

Class: D1 agonists
MOA: Activates D1 receptors and increases cAMP levels which can cause vasodilation, lowering BP. No AR activity

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24
Q

DOPA, carbidopa

A

Used in treatment of Parkinson’s Disease. Leads to production of dopamine from DOPA.

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25
Cocaine
Blocks vasopressor response to tyramine and potentiates response to NE
26
Methamphetamine, Adderall, Cocaine, Pseudoephedrine
Class: Amphetamines MOA: Blocks the uptake of NE and can stimulate both aARs and bARs causing increase in BP, decrease in HR, elevate cAMP in brain
27
mAChR and nAChR agonists (except _____, not an agonist at nAChR)
Choline esters (Carbachol, Bethanechol*, Bethanecholamine, ACh) *Bethanechol not an agonist at nAchR
28
Mimics choline esters, relatively selective for mAChRs except ______ which also activates nAChRs.
Cholinomimetic Alkaloids (Muscarine, Arecoline*, Pilocarpine, Oxotremorine, Aceclidine) *Arecoline activates mAChRs AND nAChRs
29
Reversible inhibition of mAChRs, block parasympathetic stimulation
Antimuscarinic drugs (Belladonna)
30
Antagonists to the mAChR and the nAChR
Quaternary Muscarinic Antagonists (N-methylatropine, Ipratropium, Scopolamine)
31
Competitively inhibit binding of ACh, more commonly in mAChRs, less so in nAChRs
Anticholinergics (Atropine, Diphenhydramine (Benadryl), tricyclics, Scopolamine (anti mAChRs) Curare, Hexamethonium (anti nAChRs))
32
Cholinometric effects at both nicotinic and muscarinic synapses by inhibiting AChE
Anticholinesterases (Physostigmine, Neostigmine)
33
Mostly selective for b2ARs, will stimulate cAMP and PKA. Relaxation of VSM, bronchodilators, can delay labor (______), some have cardio effects
b2AR agonists (Albuterol, Ritodrine*, Tertbutaline, Salmeterol) *Ritodrine can delay labor
34
One isomer is an a1 agonist, the other an a1 antagonist. b1AR antagonist, increases heart rate
Dobutamine
35
Activates D1 receptors and increases cAMP levels which can cause vasodilation, lowering BP. No AR activity
Fenoldopam
36
Blocks the uptake of NE and can stimulate both aARs and bARs causing increase in BP, decrease in HR, elevate cAMP in brain
Amphetamines (Methamphetamine, Adderall, Cocaine, Pseudoephedrine)
37
Phenoxybenzamine
Class: Covalent nonselective aAR antagonists MOA: Blocks aAR activation, both a1AR (Gaq) and a2AR (Gai)
38
Phentolamine
Class: Noncovalent nonselective aAR antagonist MOA: Blocks aAR activation, both a1AR (Gaq) and a2AR (Gai)
39
Prazosin, terazosin
Class: a1AR selective antagonist MOA: Blocks a1AR activation
40
Yohimbine
Class: a2AR selective antagonist MOA: Stimulates production of NO, causes vasodilation and erections
41
Propranolol, timolol, nadolol
Class: Nonselective bAR antagonists MOA: Blocks bARs in the heart, decreases cardiac output and renin secretion from kidney
42
Atenolol, Metroprolol, Esmolol
Class: b1AR selective antagonists MOA: Blocks b1AR activation
43
Butozamine
Class: b2AR selective antagonists MOA: Blocks b2AR activation
44
Labetalol
Class: Mixed AR antagonist MOA: Nonselective bAR antagonist, a1AR selective antagonist
45
a-Methyldopa
Converted in nerve terminal to a-methylnorepinephrine, which is an a2AR agonist and acts in CNS to decrease sympathetic outflow. Used to treat hypertension
46
Hydrochlorothiazide
Class: Thiazide MOA: inhibits the Na+/Cl- cotransporter which decreases Na+/Cl- reabsorption, increase Ca2+ reabsorption, K+ excretion. Can decrease systolic blood pressure, decrease afterload Toxicity: Hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlipidemia, hyperuricemia, allergic reactions , ineffective with low GFR
47
Furosemide
Class: Loop MOA: inhibits the Na+/K+/2Cl- transporter by binding Cl- site, preventing salts from being reabsorbed which prevents H2O reabsorption Toxicity: Hypokalemic metabolic alkalosis, hearing loss/ringing in ears (reversible), hyperuricemia, hypomagnesemia, hyponatremia, allergic reactions
48
Acetazolamide
Class: Carbonic anhydrase inhibitor MOA: Inhibits enzyme carbonic anhydrase, which would decrease bicarbonate reabsorption, increase Cl- excretion Toxicity: Hyperchloremic metabolic acidosis, Ca2+ renal stones, pins and needles under skin, sulfa allergy, fatigue and drowsiness
49
Mannitol
Class: Osmotic MOA: Increase in osmotic pressure in PT and TDLOH, decrease passive reabsorption of water, increased water and Na+ excretion. Activity dependent on development of osmotic pressure Toxicity: Pulmonary edema, headache, nausea, vomiting, dehydration
50
Amiloride/Spironolactone
Class: K+ sparing MOA: inhibits Na+ channel in the CD. Spironolactone inhibits aldosterone receptor in the CD, decreasing Na+ pump expression/activity Toxicity: Antiandrogen effects with spironolactone, hyperkalemia with Na+ channel blockers and aldosterone receptor antagonists
51
Tolvaptan
Class: V2R antagonist MOA: Inhibits V2 vasopressin receptor in DCT and CT, decrease aquaporin-2 insertion into apical membrane, increase water excretion Toxicity: Nephrogenic diabetes, liver damage with prolonged use
52
Blocks aAR activation, both a1AR (Gaq) and a2AR (Gai)
Covalent nonselective aAR antagonists (Phenoxybenzamine) Noncovalent nonselective aAR antagonist (Phentolamine)
53
Blocks a1AR activation
a1AR selective antagonist (Prazosin, terazosin)
54
Stimulates production of NO, causes vasodilation and erections
a2AR selective antagonist (Yohimbine)
55
Blocks bARs in the heart, decreases cardiac output and renin secretion from kidney
Nonselective bAR antagonists (Propranolol, timolol, nadolol)
56
Blocks b1AR activation
b1AR selective antagonists (metoprolol, atenolol, esmolol)
57
Blocks b2AR activation
b2AR selective antagonists (Butozamine)
58
Nonselective bAR ntagonist, a1AR selective antagonist
Mixed AR antagonist (Labetolol)
59
Converted in nerve terminal to a-methylnorepinephrine, which is an a2AR agonist and acts in CNS to decrease sympathetic outflow. Used to treat hypertension
a-Methyldopa
60
Inhibits the Na+/Cl- cotransporter which decreases Na+/Cl- reabsorption, increase Ca2+ reabsorption, K+ excretion. Can decrease systolic blood pressure, decrease afterload
Thiazides (Hydrochlorothiazide)
61
Inhibits the Na+/K+/2Cl- transporter by binding Cl- site, preventing salts from being reabsorbed which prevents H2O reabsorption
Loop diuretics (Furosemide)
62
Inhibits enzyme carbonic anhydrase, which would decrease bicarbonate reabsorption, increase Cl- excretion
Carbonic anhydrase inhibitor (Acetazolamide)
63
Increase in osmotic pressure in PT and TDLOH, decrease passive reabsorption of water, increased water and Na+ excretion. Activity dependent on development of osmotic pressure
Osmotic (Mannitol)
64
Inhibits Na+ channel in the CD Inhibits aldosterone receptor in the CD, decreasing Na+ pump expression/activity
K+ sparing (Amiloride, Spironolactone)
65
Inhibits V2 vasopressin receptor in DCT and CT, decrease aquaporin-2 insertion into apical membrane, increase water excretion
V2 receptor antagonist (Tolvaptan)

PHCOL 402 (5 decks)

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