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Pharm II Exam 1 > MOA > Flashcards

MOA Flashcards

1
Q

How do local anesthetics work?

A

wait until Na channel is activated and M gate opens up and allows lipophilic local anesthetic in and produced blockage of Na channel
can also come in during inactivated state

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2
Q

Diazepam

A

binds to inhibitory GABAa receptors and increases affinity for transmitter gaba then the transmitters open up allowing calcium in and hyperpolarizing neurons and decreasing CNS excitation

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3
Q

Clonidine

A

activates alpha 2 adrenergic receptors (AKA Mu opioid receptor) on C fiber terminals and reduces substance P release in dorsal horn and reduces pain transmission

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4
Q

How does clonidine work as an adjunct with LA?

A

combined with local anesthetic and stimulates alpha 2 receptors on termini which inhibits neurotransmitter release from fibers leading to pain attenuation

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5
Q

Benzocaine,

Procaine (Novocaine)

A

Block activated and inactivated states of the VGSC; use dependent blockade

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6
Q

Cocaine

A

Block activated and inactivated states of the VGSC; use dependent blockade

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7
Q

Lidocaine, Ropivacaine

A

Block activated and inactivated states of the VGSC; use dependent blockade

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8
Q

Epinephrine

A

Activate α1 adrenergic receptors on smooth muscle vasculature

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9
Q

Clonidine

A

Activate presynaptic α2 adrenergic receptors on C- and Adelta fibers; prevents neurotransmitter release

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10
Q

Diazepam (Valium)

A

Activate GABA-A receptors in CNS

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11
Q

Terodotoxin (TTX)

A

Binds to outer pore of Na channel and blocks Na entery by steric hinderance

Binds regardless to state the Na channel is in

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12
Q

Nitrous Oxide

A

Inhibit Kainate and NMDA receptors

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13
Q

Isoflurane

A

Potentiate GABA(A)R

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14
Q

Sevoflurane

A

Potentiate GABA(A)R

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15
Q

Propofol

A

Potentiate GABA(A)R

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16
Q

Etomidate

A

Potentiate GABA(A)R

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17
Q

Ketamine

A

Inhibits NMDA receptor

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18
Q

Sodium Thiopental

A

Potentiate GABA(A)R

↑ length of time Cl- channels remain open

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19
Q

Benzodiazepines

A

↑ affinity of GABA for GABA(A)r

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20
Q

Ondansetrone

A

5HT3 antagonist

21
Q

Diazepam (Valium®)

A

Long acting benzodiazepine that activates GABA-A(r) in CNS

Benzodiazepines act by ↑ affinity of endogenous GABA to GABA-AR

22
Q

Clonidine

A

Clonidine activates α2 adrenergic receptors in CNS to ↓ sympathetic outflow

23
Q

Propranolol

A

Propranolol blocks β adrenergic receptors in CNS to decrease sympathetic outflow

24
Q

Disulfiram

A

Inhibits acetaldehyde dehydrogenase (ALDH) → accumulation of acetaldehyde upon alcohol consumption

Acetaldehyde induces N/V, HA, hypotension

25
Q

Naltrexone

A

Inhibits mu opioid receptors in ventral tegmental region (VTA) of brain; long acting antagonist

26
Q

Naloxone

A

Narcan test

Inhibits mu opioid receptors in ventral tegmental region (VTA) of brain; short acting antagonist

27
Q

Acamprosate, Topiramate

A

Anti-craving mechanism unknown.

These drugs treat epilepsy by ↑ activity of inhibitory GABA-A(r) and inhibiting excitatory glutamatergic receptor activity

28
Q

Fomepizole, Ethanol

A

Binds with high affinity to alcohol dehydrogenase (ADH) thereby preventing metabolism of methanol and ethylene glycol to toxic metabolites

29
Q

N- acetylcysteine (NAC)

A

Neutralizes reactive intermediates resulting from metabolism of acetaminophen by P450 enzymes CYP2E1, CYP1A2 and CYP3A4

30
Q

Ribavirin (HCV)

A

Guanosine analog that is phosphorylated intracellularly by host cell enzymes
→ blocks capping of viral mRNA and inhibits viral RNA-dependent polymerase → mutations in RNA (no longer functional)

31
Q

Pegylated (Peg) Interferon

A

Induces intracellular signals → inhibition of viral penetration/translation/transcription/protein processing/maturatio and release

32
Q

Sofosbuvir

Sovaldi

A

RNA-dependent HCV Polymerase inhibitor (NS5B inhibitors)

33
Q

Ledipasvir

A 
Blocks replication (NS5A interacts with NS5B) via preventing RNA binding to polymerase
→  Inhibits viral assembly and release
34
Q

H2 Receptor Antagonists

A

Directly block histamine-stimulated gastric acid secretion on parietal cell

35
Q

Omeprazole

A

Irreversible inhibition of parietal Cell proton pump (H+/K+ ATPase) → ↓ gastric acid secretion

Weak base accumulates in parietal cell canaliculus → protonated form of drug binds covalently to enzyme

36
Q

Antacids

A

Weak bases that are poorly absorbed (so stay in GI lumen) and directly neutralize stomach acid

37
Q

Sucralfate

A

Form paste like get at low pH that adheres to positively charged proteins of epithelial cells as well as ulcer craters to form coating that protects cells against acid

38
Q

Bismuth Subsalicylate

A

Binds selectively to ulcers to protect against acid and pepsin

39
Q

Misoprostol

A

PGE1 analog

Inhibits acid secretion (ECL and possibly parietal cell)

Augments mucus and HCO3-secretion

40
Q

Metoclopramide

A

Prokinetic
– enhances ACh release in myenteric plexus, ↑ intestinal smooth
muscle response to Ach

41
Q

Ondansetron

A

IV/po

little or no effects on muscarinic or dopaminergic receptors

42
Q

Infliximab (Remicade)

A

Binds to TNF-alpha to block its inflammatory effects at TNF receptors

43
Q

Sulfasalazine

A

Important to be delivered topical onto intestinal wall because systemic does not work

44
Q

Alosetron

A

5-HT3 receptor antagonist

↓ colonic motility via enteric and CNS blockade of 5-HT3 receptors

45
Q

Loperamide

A

Slows intensional transit due to stimulation of my opioid receptors in intestinal smooth muscle

46
Q

Mg(OH)2

A

Osmotic gradient ↑ water movement into lumen, stimulates peristalsis

47
Q

Linaclotide

A

Activation of the CFTR; via cGMP ↑ intestinal fluid secretion→ ↑ number of bowel movements

48
Q

Lubiprostone

A

Directly activates Cl channel

↑ intestinal fluid secretion → ↑ number of bowel mvts

Pharm II Exam 1 (7 decks)

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