Block 3 Drugs Flashcards

1
Q

Atropine

A

Classification: muscarinic antagonist

Main clinical applications: preanesthetic to prevent respiratory secretions; sinus bradycardia, blockade of excessive muscarinic receptor activation

  • *Pharmacodynamics:** Mechanisms/Sites of Action
  • heart: high doses can result in tachycardia
  • lungs: bronchodilation; decreased secretion
  • GI tract: decreased motility
  • glands: decreased salivation and sweating

Adverse Effects: dry mouth, urinary retention, tachycardia. Contraindicated in glaucoma, prostatic hypertrophy, heart disease.

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2
Q

Buspirone

A

Classification: 5-HT1A partial agonist

Main clinical applications: used for treatment of functional dyspepsia with impaired accommodation; CNS application - used as an anxiolytic for the treatment of anxiety disorders

  • *Pharmacodynamics: Mechanisms/Sites of action**
  • induces relaxation of the proximal stomach; alleviates dyspeptic symptoms, and is associated with and enhancement of accommodation to a meal

Adverse Effects: dizziness, headache, nausea (infrequent)

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3
Q

Cimetidine

A

Classification: histamine H2 receptor antagonist

Main clinical applications: used for duodenal/gastric ulcer, hypersecretion of acid, GERD

  • *Pharmacodynamics: Mechanisms/Sites of Action**
  • histamine H2 receptor antagonist that inhibits acid secretion into stomach

Adverse Effects: diarrhea, dizziness, rash, headache, confusion

Relevant Pharmacokinetics: it is a known inhibitor of many isozymes of the cytochrome P450 enzyme system (eg CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4)

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4
Q

Erythromycin

A

Classification: macrolide antibiotic
motilin agonist

Main clinical aplications: treat respiratory tract and soft tissue infections; used for treatment of gastroparesis due to its pro-motility effects

  • *Pharmacodynamics: Mechanism/Sites of action**
  • binds to the 50 s ribosomal subunit, inhibiting bacterial protein synthesis
  • useful in treating gastroparesis
  • considered a motilin receptor agonist able to stimulate gastrointestinal motility by a combination of direct muscular and indirect neurotransmitter effects

Adverse Effects: GI upset

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5
Q

Fluoxetine

A

Classification: SSRI antidepressent

Main clinical applications: used for treatment of depression, obsessive compuslive disorder, bulimia nervosa

  • *Pharmacodynamics: Mechanism/Sites of action**
  • selective serotonin reuptake inhibitor that blocks the uptake of serotonin at all SERT sites, both in the CNS and PNS

Adverse Effects: GI discomfort, nausea, headache, nervousness, insomnia, anxiety or diarrhea

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6
Q

Metoclopramide

A

Classification: prokinetic drug

Main clinical applications: used for treatment of reflux esophagitis, pre-op gastric emptying, reduces chemotherapy - induced nausea; used for its antiemetic and prokinetic properties

  • *Pharmacodynamics: Mechanism/Sites of action**
  • acts as a 5-HT3 antagonist and a 5-HT4 agonist. Indirectly effects increases in ACh release in gut. Dopamine D2 receptor antagonist in CNS and PNS.

Adverse Effects: diarrhea, drowsiness, depression

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7
Q

Misoprostol

A

Classification: a synthetic, oral prostaglandin E1 analog

Main clinical applications: used for and is commonly believed to be effective for prevention of gastric and duodenal ulcers secondary to use of nonsteroidal antiinflammatory drugs (NSAIDs) although currently it is indicated only for the prevention of gastric ulcers

  • *Pharmacodynamics: Mechanism/Sites of action**
  • exerts a mucosal protectant effect that may contribute to its effectiveness in treating ulcers. It has been suggested that the cytoprotective effect is secondary to mucus and bicarbonate secretion, prevention of mucus bilayer disruption, reduction of backflow of hydrogen ions and regulation of mucosal blood flow

Adverse Effects: diarrhea, abdominal pain, dyspepsia

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8
Q

Neostigmine

A

Classification: carbamate-type peripheral cholinesterase inhibitor

Main clinical applications: myasthenia gravis diagnosis and treatment, paralytic ileus (increases gastric motility), lack of bladder tone, reversal of neuromuscular blockade following anesthesia

  • *Pharmacodynamics: Mechanism/Sites of action**
  • carbamate type acetylcholinesterase inhibitor in the periphery

Adverse Effects: bowel craps, diarrhea

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9
Q

Octreotide

A

Classification: synthetic analog of somatostatin

Main clinical applications: used for treatment of diarrhea and other symptoms of abdominal illness; also for other medical conditions such as intestinal tumors vasoactive intestinal peptide tumors, metastatic carcinoid tumors, acromegaly, variceal bleeding, orthostatic hypotension

  • *Pharmacodynamics: Mechanism/Sites of action**
  • antidiarrheal
  • mimics somatostatin pharmacologically; inhibits gastric acid and pepsin secretion; reduces gastrointestinal motility and inhibits contraction of the gallbladder and bile flow; reduces liver blood flow

Adverse Effects: abdominal cramps and nausea common

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10
Q

Omeprazole

A

Classification: proton pump inhibitor (PPI)
other PPIs: lansoprazole, rabeprazole, pantoprazole, esomeprazole

Main clinical applications: used for gastroesophageal reflux disease, duodenal ulcer, hypersecretory states (Zollinger-Ellison syndrome)

  • *Pharmacodynamic: Mechanism/Site of action**
  • blocks secretion of acid by irreversibly inhibiting the H+/K+ ATPase in the parietal cell

Adverse effects: few side effects, constipation

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11
Q

Ondansetron

A

Classification: 5-HT3 antagonist (same as granisetron)

Main clinical applications: prophylactic administration used for treatment of vomiting and nausea following chemotherapy; also for vomiting postoperatively

  • *Pharmacodynamics: Mechanism/Sites of action**
  • 5-HT3 receptor antagonist; its effect both in periphery and chemotrigger zone (CTZ) - an area of the brain which receives inputs from blood-borne drugs or hormones

Adverse Effects: headache, constipation

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12
Q

Ranitidine

A

Classification: histamine H2 receptor antagonist

Main clinical applications: used for treatment of duodenal/gastric ulcer, hypersecretion of acid, GERD

  • *Pharmacodynamics: Mechanism/Sites of action:**
  • histamine H2 receptor antagonist that inhibits secretion of acid in the stomach; more potent that cimetidine

Adverse Effects: diarrhea, dizziness, rash, headache, confusion; fewer side effects than cimetidine

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13
Q

Sumatriptan

A

Classification: 5-HT1B/1D agonist and an agonist at 5-HT1P receptors

Main clinical applications: used for treatment of functional dyspepsia with impaired accommodation; acute migraine, cluster headache attacks

  • *Pharmacodynamics: Mechanism/Sites of action**
  • its peripheral actions include fundal relaxation and reductions in antral motility; as a 5-HT1B/1D agonist it causes vasoconstriction

Adverse Effects: may initially cause flushing, dizziness, weakness, nausea, drowsiness, stiffness, or feelings of tingling

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14
Q

Sucralfate

A

Classification: cytoprotectant; mucosal coating agent

Main clinical applications: treatment of gastric, duodenal, stress ulcers

  • *Pharmacodynamics: Mechanism/Sites of action**
  • acts locally (not systematically) to complex with proteins at ulcer site; forms a protective, viscous, adhesive barrier on the surface of intact mucosa of stomach and duodenum; inhibits pepsin activity

Adverse Effects: constipation

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15
Q

Antacids

A

Classification: (Al)OH3, Mg(OH)2, CaCO3; Alka-Seltzer (acetylsalicylic acid, sodium bicarbondate (NaHCO3), and citric acid) also simethicone

Main clinical applications: antacids neutralize acid in stomach

Pharmacodynamics: Mechanism/Sites of action
- Neutralization by acid-base interactions or binding of H+
often included in these preparations - simethicone: antiflatulent agent/ surfactant that may reduce flatulence or belching by decreasing foaming (change in surface tension of gas bubbles which otherwise quickly coalesce)

Adverse Effects: constipation

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16
Q

Oxybutynin (Ditropan)

A

Classification: anticholinergic, antimuscarinic

Main clinical applications: bladder muscle relaxant

  • *Pharmacodynamics:** Mechanism/Sites of action
  • surpresses the urge to void; inhibits voluntary detrussor muscle contractions cause by detrusor muscle instability (non-neurogenic) or detrusor muscle hyperreflexia. Reduced contractions allow the bladder to relax and increase its visceral capacity.

Adverse Effects: since its a non-selective antimuscarinic, side effects are consistent with anticholinergic actions in the CNS, glands, and GI tract (dry eyes, hyposalivation, decreased gastric motility, constipation, headache, sleepiness)

17
Q

Tolterodine (Detrol)

A

Classification: anticholinergic, antimuscarinic

Main clinical applications: bladder muscle relaxant

  • *Pharmacodynamics: Mechanism/Sites of action**
  • suppresses the urge to void; inhibits involuntary detrusor muscle contractions cause by detrusor muscle instability (non-neurogenic) or detrusor muscle hyperreflexia. Reduced contractions allow the bladder to relax and increase its visceral capacity.

Adverse Effects: since its a non-selective antimuscarinic, side effects consistent with anticholinergic actions in CNS, glands, GI tract (dry eyes, hyposalivation, decreased gastric motility, constipation, headache, sleepines)

18
Q

Amitriptyline (Elavil)

A

Classification: tricyclic antidepressant (TCA)

Main clinical applications: has multiple applications (ie bladder relaxant)

  • *Pharmacodynamics: Mechanism/Sites of action**
  • acts as a reuptake blocker at NE and 5-HT nerve terminal, resulting in increases of NE and 5-HT extraneuronal concentrations. For pharmacological actions related to urine storage, the drug decreases bladder contractility due to its antimuscarinic effects.

Adverse Effects: has anticholinergic effects (eg drowsiness, dizziness, dry mouth, blurred vision, constipation, fast heartbeat, nausea, vomiting); also alpha 1 antagonist and antihistamine (H1) actions

19
Q

Alpha Adrenergic Antagonists

(terazosin, doxazosin, tamsulosin (Flomax), alfuzosin (Uroxatral))

A

Classification: selective antagonist at alpha1-receptors

Main clinical applications: used for treatment of benign prostatic hyperplasia (BPH); Meta-analyses have shown alfuzosin, doxazosin, tamsulosin, and terazosin to be comparable in the treatment of BPH

  • *Pharmacodyanmics:** Mechanism/Sites of action
  • relaxes the smooth muscle of the prostate and bladder neck to facilitate bladder emptying

Adverse Effects: effects associatd with blockade of alpha1-receptors - eg hypotension, ejaculation dysfunction

20
Q

Vasodilators

(sildenafil (Viagra, Revatio), vardenafil (Levitra), tadalafil (Cialis))

A

Classification: vasodilator

Main clinical appliations: used to treat male erectile dysfunction (impotence) and pulmonary arterial hypertension

  • *Pharmacodynamics: Mechanism/Sites of action**
  • inhibitor of cGMP specific phosphodiesterase type 5 (PDE5). part of the physiological process of erection involves the parasympathetic nervous system causing the release of nitric oxide (NO) in the corpus cavernosum of the penis. NO binds to the enzyme guanylate cyclase which results in increased levels of cyclic guanosine monophosphate (cGMP). This leads to smooth muscle relaxation (vasodilation) in the corpus cavernosum, resulting in increased inflow of blood and an erection. PDE5 inhibitors inhibit degradation of cGMP in the corpus cavernosum, thereby prolonging cGMP action.
  • no effect in the absence of sexual stimulation

Adverse Effects: headache, flushing, dyspepsia, priapism

21
Q

5-alpha-reductase inhibitor

(finasteride (Proscar), dutasteride (Avodart))

A

Classification: 5-alpha-reductase inhibitor

Main clinical applications: for treatment of symptomatic benign prostatic hyperplasia (BPH)

Pharmacodynamics: Mechanism/Sites of action
- reduction in prostate hyperplasia;
a competitive, specific inhibitor of type II 5-alpha-reductase, an intracellular enzyme that converts testosterone to dihydrotestosterone
In benign prostatic hyperplasia, dihydrotestosterone acts as a potent cellular androgen and promotes prostate growth. Thus, inhibiting the reductase enzyme lowers dihydrotestosterone levels which reduces excessive prostate growth.

Adverse Effects: sexual dysfunction; also gynecomastia

22
Q

Colchicine

A

Classification: antiinflammatory drug for gout

Main clinical applications: primarily for the treatment of acute gout attacks

  • *Pharmacodynamics: Mechanism/Sites of action**
  • binds to proteins in microtubules of neutrophils; That action inhibits neutrophil migration into the joint area and interferes with the inflammatory response to urate crystal deposition (note: no analgesic effects, no effects on uric acid clearance)

Adverse Effects: abdominal pain; vomiting and/or diarrhea

23
Q

Allopurinol

A

Classification: antigout drug - xanthine oxidase inhibitor

Main clinical applications: used for treatment of chronic gout

  • *Pharmacodynamics: Mechanism/Sites of action**
  • action inhibits the enzyme xanthine oxidase. However, drug also acts as a muscarinic antagonist and it is this pharmacologic action that relaxes the detrusor muscle of the bladder.

Adverse Effects: most common adverse effects are dermatologic, which can be severe and sometimes fatal; should be discontinued at the first sign of a skin rash or other signs that may indicate a hypersensitivity reaction

24
Q

Probenecid

A

Classification: uricosuric drug

Main clinical applications: used to treat hyperurecemia associated with chronic gout

  • *Pharmacodynamic: Mechanism/Sites of action**
  • competitively inhibits the active reabsorption of uric acid at the proximal convoluted tubule
  • *Adverse Effects:** not associated with many adverse effects; occassionally, headache, nausea/vomiting, dizziness
    (note: not effective for acute attacks of gout and can actually aggravate inflammation if administered during the initial stages; can increase the number of acute gouty attacks occurring in the first 6-12 months of therapy)
25
Q

Sulfinpyrazone

A

Classification: uricosuric drug

Main clinical applications: used to treat chronic or intermittent gouty arthritis

  • *Pharmacodynamics:** Mechanism/Sites of action
  • inhibits reabsorption of uric acid, and therefore increases its urinary excretion and decreases its plasma concentration
  • *Adverse Effects:** gastrointestinal, avoid use in patients with peptic ulcer disease; dosage should be slowly titrated to prevent urate kidney stone formation; may worsen an acute attack due to its potent mobilization of urate stores.
    (note: not intended for the treatment of acute attacks because it lacks therapeutically useful analgesic and antiinflammatory effects)
26
Q

Disulfiram

A

Classification: management of ethanol abuse

Main clinical applications: negative-reinforcer used as a deterrent for alcohol abuse

  • *Pharmacodynamics: Mechanism/Sites of action**
  • inhibits hepatic oxidation of acetaldehyde (a metabolic of ethanol); the pharmacological effects are cause by acetaldehyde

Adverse Effects: the buildup of acetaldehyde plasma concentrations are associated with very unpleasant reactions, including headache, dyspnea, nausea, lasting from 30 min to several hours; these reactions can be followed by a deep sleep