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MS1 Drugs > Block 3 Drugs > Flashcards

Block 3 Drugs Flashcards

1
Q

Atropine

A

Muscarinic antagonist

Uses:

  • preanesthetic to prevent respiratory secretions
  • to treat sinus bradycardia
  • blockade of excessive muscarinic receptor activation

Sites of action:

  • heart - high dose can cause tachy
  • lungs - causes bronchodilation, decreased secretion
  • GI - decreased motility
  • glands - decreased salivation and sweating
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2
Q

Busiprone

A

5-HT1A partial agonist

Use:

  • treating dyspepsia (upset stomach/indigestion)
  • an anxiolytic for anxiety disorders

Mechanisms:

  • induces relaxation of proximal stomach
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3
Q

Cimetidine

A

Histamine H2 receptor antagonist

Use:

  • for duodenal/gastric ulcers
  • hypersecretion of acid
  • GERD

Mechanisms:

  • inhibits acid secretion into stomach

Notes:

  • inhibitor of many isozymes of the cytochrome P450 enzyme system (CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4)
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4
Q

Erythromycin

A

Macrolide antibiotic; motilin receptor agonist

Use:

  • treating resp. tract + soft tissue infections
  • treating gastroparesis (delayed gastric emptying) due to its pro-motility effect

Mechanisms:

  • binds to 50s ribosomal subunit thus inhibiting bacterial protein synthesis
  • as a motilin receptor agonist by direct muscular and indirect NT effects to stimulate GI motility
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5
Q

Fluoxetine

A

SSRI antidepressant

Used to treat:

  • depression
  • obsessive compulsive disorder
  • bulimia nervosa

Mechanism:

  • selective serotonin reuptake inhibitor (SSRI) at all SERT sites, in both CNS and PNS
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6
Q

Metoclopramide

A

5-HT3 antagonist; 5-HT4 agonist; dopamine D2 receptor antagonist; prokinetic drug

Use:

  • treating reflux esophagitis
  • for pre-op gastric emptying
  • reduces chemotherapy-induced nausea
  • an antiemetic
  • is prokinetic (enhances GI motility)

Mechanisms:

  • 5-HT3 antagonist
  • 5-HT4 agonist
  • Metoclopramide is a dopamine D2 receptor antagonist in CNS + PNS
  • Dopamine D2 receptors inhibit ACh release (ACh is needed for gut motility)
  • indirectly increases ACh release in gut
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7
Q

Misoprostol

A

Synthetic oral prostaglandin E1 analog

Use:

  • for preventing gastric and duodenal ulcers secondary to use of NSAIDS, but currently indicated only for prevention of gastric ulcers

Mechanism:

  • exerts a mucosal protectant effect. Its cytoprotective effect is secondary to: mucus and bicarb secretion, prevention of mucus bilayer disruption, reduction of backflow of H+, regulation of mucosal blood flow
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8
Q

Neostigmine

A

Carbamate-type peripheral cholinesterase inhibitor

Use:

  • for myasthenia gravis dx and treatment
  • paralytic ileus (neostigmine increases gastric motility)
  • lack of bladder tone
  • reversal of neuromuscular blockade following anesthesia

Notes:

  • carbamate-type acetylcholinesterase inhibitor in periphery
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9
Q

Octreotide

A

Synthetic analog of somatostatin

Use:

  • treating diarrhea, other abdominal illness
  • for intestinal tumors, vasoactive intestinal peptide tumors, metastatic carcinoid tumors, acromegaly (excess growth hormone), variceal bleeding, orthostatic hypotension

Mechanisms:

  • antidiarrheal - mimics somatostatin pharmacologically
  • inhibits gastric acid and pepsin secretion
  • reduces GI motility
  • Inhibits contraction of gallbladder and bile flow
  • reduces liver blood flow
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10
Q

Omeprazole

A

Proton pump inhibitor (PPI)

Used to treat:

  • gastroesophageal reflux disease
  • duodenal ulcer
  • hypersecretory states (Zollinger-Ellison syndrome)

Mechanism:

  • blocks acid secretion by irreversibly inhibiting the H+/K+ ATPase in parietal cells
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11
Q

Ondansetron

A

5-HT3 antagonist

Use:

  • a prophylactic used to treat nausea and vomiting following chemotherapy
  • for postoperative vomiting

Mechanism:

  • 5-HT3 serotonin receptor antagonist
  • its effects are BOTH in periphery and at chemotrigger zone (CTZ, an area of brain that receives input from blood-borne drugs or hormones)

Notes:

  • granisetron is in the same class
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12
Q

Ranitidine

A

Histamine H2 receptor antagonist

Used to treat:

  • duodenal/gastric ulcer
  • hypersecretion of acid
  • GERD (gastroesophageal reflux disease)

Mechanism:

  • inhibits secretion of acid in stomach
  • more potent than cimetidine

Notes:

  • fewer side effects of cimetidine
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13
Q

Sulcralfate

A

Cytoprotectant; mucosal coating agent

Used to treat:

  • gastric, duodenal, and stress ulcers

Mechanisms:

  • acts locally (not systemically) to complex with proteins at ulcer site
  • forms protective, viscous, adhesive barrier on surface of intact mucosa of stomach and duodenum
  • inhibits pepsin activity
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14
Q

Sumatriptan

A

5-HT1B/1D receptor and 5-HT1P receptor agonist

Used to treat:

  • functional dyspepsia with impaired accommodation
  • acute migraine
  • cluster headache attacks

Mechanism:

  • Its peripheral actions include fundal relaxation and reductions in antral motility
  • as a 5-HT1B/1D receptor agonist it causes vasoconstriction
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15
Q

Insulin

A

Always give insulin to diabetics REGARDLESS OF GLUCOSE LEVELS b/c lack of it can result in life-threatening ketoacidosis.

If glucose is low, give insulin + glucose to avoid ketoacidosis.

Insulin acts on receptors which, through a cascade, lead to increased amounts of GLUT 4 (glucose transporters) on the cell membrane.

Causes weight gain.

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16
Q

Metformin

A

First choice drug to treat Type 2 DM

It makes the liver more sensitive to insulin (“hearing aid for the liver”).

Inhibits gluconeogenesis.

Enhances GLUT 4 translocation (GLUT 4 then brings in glucose from blood into cells)

Makes people eat less.

Decreases risk of cancer.

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17
Q

Sulfonylureas (glucotrol, glipizide)

A

Treating Type 2 DM

Stimulates beta cells of the pancreas to secrete more insulin

Dr. Butler does not like this drug

18
Q

Thiazolidines (pioglitizone)

A

Treating Type 2 DM.

Enhances insulin receptor activity

Enhances GLUT4 translocation in fat cells.

HOWEVER, risk for MI and stroke are the same

19
Q

Glitazones

A

Treating Type 2 DM.

Enhances how insulin works at the muscle, but has side-effects

20
Q

Glucagon like peptide (GLP-1)

A
21
Q

Incretin mimetics (exenatide)

A

For treating diabetes.

Incretin, a naturally occuring hormone secreted by intestines in response to food intake, acts on pancreas to stimulate secretion of glucose-dependent insulin.

DOES NOT CAUSE weight gain. Is associated with weight loss. This is a good thing for Type 2 DM.

22
Q

Dipeptidyl peptidase-4 (DPP-4) inhibitors (sitagliptin)

A

For treating diabetes.

DPP-4 degrades incretin.

Increases incretin available to respond to elevated glucose levels by limiting rapid degradation of incretins by DPP-4 enzyme.

DOES NOT cause weight gain.

23
Q

Oxybutynin (Ditropan)

A

Anticholinergic, antimuscarinic (non-selective)

Use:

  • Is a bladder muscle relaxant, it suppresses urge to void

Mechanisms of Action:

  • inhibits involuntary detrusor muscle contractions caused by detrusor muscle instability (non-neurogenic) or detruso muscle hyperreflexia. Reduced contractions allow the bladder to relax and increase its visceral capacity

Notes:

  • There are cholinergic muscarinic m2 and m3 receptors on the detrusor muscle of the urinary bladder wall
24
Q

Tolderodine (Detrol)

A

Anticholinergic, antimuscarinic

Use:

  • a bladder muscle relaxant (same class as oxybutynin)

Mechanism of Action:

  • Same as oxybutynin

Note:

  • There are cholinergic muscarinic m2 and m3 receptors on the detrusor muscle of the urinary bladder wall
25
Q

Amitriptyline (Elavil)

A

Tricyclic Antidepressant

Use:

  • has multiple applications - e.g. as a bladder relaxant

Mechanism:

  • acts as a reuptake blocker at NE and 5-HT nerve terminal resulting in increases of NE and 5-HT extraneuronal concentrations.
  • Decreases bladder contractility due to its antimuscarinic effects.

Note:

  • bladder has cholinergic m2 and m3 receptors.
26
Q

5-alpha-reductase inhibitors (same class as finasteride (Proscar), dutasteride (Avodart))

A

5-alpha-reductase inhibitor

Use:

  • treating symptomatic benign prostatic hypertrophy (BPH)

Mechanism:

  • Reduction in prostate hyperplasia; a competitive specific inhibitor of type II 5-alpha-reductase, an intracellular enzyme that converts testosterone to dihydrotestosterone. In BPH, dihydrotestosterone acts as a potent cellular androgen and promotes prostate growth. Thus, inhibiting the reductase enzyme lowers dihydrotestosterone levels which reduces excessive prostate growth.
27
Q

Vasodilators

Same class as: sildenafil (Viagra, Revatio), vardenafil (Levitra), tadalafil (Cialis)

A

Vasodilator

Use:

  • treating male erectile dysfunction (impotence) and pulmonary arterial HTN

Mechanism:

  • inhibitor of cGMP specific phosphodiesterase type 5 (PDE 5).
  • PDE 5 inhibitors inhibit degradation of cGMP in the corpus cavernosum, thereby prolonging cGMP action (see below)

Note:

  • Part of the process of erection involves the parasympathetic nervous system causing the relase of nitric oxide (NO) in the corpus cavernosum of the penis. NO binds to the enzyme guanylate cyclase which results in increased levels of cGMP. This leads to smooth muscle relaxation (vasodilation) in the corpus cavernosum resulting in increased inflow of blood and an erection. Breakdown of cGMP by PDE 5 limits the degree of vasodilatation and limits erection of the penis.
28
Q

Alpha-Adrenergic Antagonists

Same class: terazosin, doxazosin, tamsulosin (Flomax), alfuzosin (Uroxatral)

A

Selective alpha-1 receptor antagonist

Use:

  • for treatment of benign prostatic hyperplasia (BPH)
  • Alfuzosin, doxazosin, tamsulosin, terazosin are all comparable in the treatment of BPH.

Mechanism:

  • relaxes the smooth muscle of the prostate and bladder neck to facilitate bladder emptying.
29
Q

Essure

A

Nonsurgical female sterilization

Hysteroscopic placement of metallic microcoils in both proximal fallopian tubes. Fibrotic response occludes the tubes in 3 (96%)-6 months (100%).

30
Q

Adiana

A

Nonsurgical female sterilization

Hysteroscopic placement of polymer matrix in both proximal fallopian tubes. Uses radiofrequency energy to stimulate vascular tissue growth into the polymer matrix.

Effectiveness: 98.9%

31
Q

Copper T

Progestin IUD (Progestasert, Mirena)

A

Intrauterine Device

Copper T - hormonally inert (?) and lasts for 10 years

Progestasert (1 year) and Mirena (5 years) release a synthetic progesterone called levonorgestrel

32
Q

Depo-Provera, DMPA-104

A

Injectable IM or SQ

Progestin, 4 shots per year.

Targets pituitary LH and FSH.

33
Q

Implanon

A

Progestin Implant (SQ)

Lasts for 3 years. Targets pituitary LH and FSH

34
Q

OrthoEvra

A

Transdermal patch

Estrogen + progesterone, weekly.

Targets pituitary LH and FSH.

35
Q

Nuvaring

A

Vaginal ring

Estrogen + progesterone, monthly.

Targets pituitary LH and FSH.

36
Q

Preven

A

Emergency Contraceptive

Two doses of estrogen + progestin 12 hours apart.

37
Q

Plan B (and Plan B one-step)

A

Progestin-only emergency contraceptive that prevents LH surge and subsequent ovulation if taken prior to these events.

Plan B is two doese of progestin 12 hours apart

Plan B one-step is one high dose of progestin

38
Q

RU-486 (aka Mifepristone)

A

Emergency contraceptive

Progesterone receptor antagonist

One dose, not in clinical use

100% effective

39
Q

EllaOne

A

Emergency Contraceptive - selective progesterone receptor modulator (SPRM)

Delays ovulation via LH inhibition.

Single 30 mg dose effective up to 5 days/120 hours after intercourse

40
Q
A

MS1 Drugs (2 decks)

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