MOA

Question 1

How do local anesthetics work?

Answer 1

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

Question 2

Diazepam

Answer 2

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

Question 3

Clonidine

Answer 3

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

Question 4

How does clonidine work as an adjunct with LA?

Answer 4

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

Question 5

Benzocaine,

Procaine (Novocaine)

Answer 5

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

Question 6

Cocaine

Answer 6

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

Question 7

Lidocaine, Ropivacaine

Answer 7

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

Question 8

Epinephrine

Answer 8

Activate α1 adrenergic receptors on smooth muscle vasculature

Question 9

Clonidine

Answer 9

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

Question 10

Diazepam (Valium)

Answer 10

Activate GABA-A receptors in CNS

Question 11

Terodotoxin (TTX)

Answer 11

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

Binds regardless to state the Na channel is in

Question 12

Nitrous Oxide

Answer 12

Inhibit Kainate and NMDA receptors

Question 13

Isoflurane

Answer 13

Potentiate GABA(A)R

Question 14

Sevoflurane

Answer 14

Potentiate GABA(A)R

Question 15

Propofol

Answer 15

Potentiate GABA(A)R

Question 16

Etomidate

Answer 16

Potentiate GABA(A)R

Question 17

Ketamine

Answer 17

Inhibits NMDA receptor

Question 18

Sodium Thiopental

Answer 18

Potentiate GABA(A)R

↑ length of time Cl- channels remain open

Question 19

Benzodiazepines

Answer 19

↑ affinity of GABA for GABA(A)r

Question 20

Ondansetrone

Answer 20

5HT3 antagonist

Question 21

Diazepam (Valium®)

Answer 21

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

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

Question 22

Clonidine

Answer 22

Clonidine activates α2 adrenergic receptors in CNS to ↓ sympathetic outflow

Question 23

Propranolol

Answer 23

Propranolol blocks β adrenergic receptors in CNS to decrease sympathetic outflow

Question 24

Disulfiram

Answer 24

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

Acetaldehyde induces N/V, HA, hypotension

Question 25

Naltrexone

Answer 25

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

Question 26

Naloxone

Answer 26

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

Question 27

Acamprosate, Topiramate

Answer 27

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

Question 28

Fomepizole, Ethanol

Answer 28

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

Question 29

N- acetylcysteine (NAC)

Answer 29

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

Question 30

Ribavirin (HCV)

Answer 30

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)

Question 31

Pegylated (Peg) Interferon

Answer 31

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

Question 32

Sofosbuvir | Sovaldi

Answer 32

RNA-dependent HCV Polymerase inhibitor (NS5B inhibitors)

Question 33

Ledipasvir

Answer 33

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

Question 34

H2 Receptor Antagonists

Answer 34

Directly block histamine-stimulated gastric acid secretion on parietal cell

Question 35

Omeprazole

Answer 35

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

Question 36

Antacids

Answer 36

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

Question 37

Sucralfate

Answer 37

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

Question 38

Bismuth Subsalicylate

Answer 38

Binds selectively to ulcers to protect against acid and pepsin

Question 39

Misoprostol

Answer 39

PGE1 analog Inhibits acid secretion (ECL and possibly parietal cell) Augments mucus and HCO3-secretion

Question 40

Metoclopramide

Answer 40

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

Question 41

Ondansetron

Answer 41

IV/po little or no effects on muscarinic or dopaminergic receptors

Question 42

Infliximab (Remicade)

Answer 42

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

Question 43

Sulfasalazine

Answer 43

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

Question 44

Alosetron

Answer 44

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

Question 45

Loperamide

Answer 45

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

Question 46

Mg(OH)2

Answer 46

Osmotic gradient ↑ water movement into lumen, stimulates peristalsis

Question 47

Linaclotide

Answer 47

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

Question 48

Lubiprostone

Answer 48

Directly activates Cl channel ↑ intestinal fluid secretion → ↑ number of bowel mvts