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Flashcards in Drugs Deck (56)
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1
Q

Isoniazid

A

Anti-tuberculosis drug metabolized by N-acetyltransferase-2

2
Q

Anti-depressants

A

Metabolized by CYP2D6

3
Q

Omeprazole, Phenytoin, Clopidogrel

A

Metabolized by CYP2C19

4
Q

Warfarin

A

Metabolized by CYP2C9

- A vitamin K antagonist that inhibits Vitamin K epoxide reductase complex (VKORC1)

5
Q

Succinylcholine

A

a depolarizing muscle relaxant - treatment affected by pseudocholinesterase polymorphism

6
Q

Mercaptopurine

A

Bone marrow suppression in cancer treatment

- treatment affected by TPMPT polymorphism

7
Q

Digoxin

A

Cardiac glycoside - Treatment affected by P-glycoprotein polymorphism

8
Q
Norepinephrine
Classification:
Receptor activity:
Cardiovascular effects:
Therapeutic Uses:
A

Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor activity: α1, (α2, β1)
Cardiovascular effects: Peripheral vasoconstriction - increase PVR; Increase BP; reflex bradycardia
Therapeutic Uses: Used as vasoconstrictor under intensive care situations (shock); Increase BP during reduced sympathetic tone

9
Q
Epinephrine
Classification:
Receptor activity:
Cardiovascular effects:
Respiratory:
Metabolic:
Therapeutic Uses:
A

Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor activity: α1, α2, β1, β2
Cardiovascular effects: Increase HR, contractile force, CO; Increase SBP, decrease DBP; Decrease PVR; Constriction of vascular beds but dilation of skeletal muscle vessels
Respiratory: Bronchodilation
Metabolic: Hyperglycemia and Lypolysis
Therapeutic Uses: Rapid relief of hypersensitivity reactions to drugs and other allergens; Co administered with local anesthetics to increase duration of action

10
Q
Isoproterenol
Classification:
Receptor activity:
Cardiovascular effects:
Respiratory:
Therapeutic Uses:
A

Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor activity: β1, β2
Cardiovascular effects: Decrease peripheral resistance; increase HR, contractile force, CO; Decrease mean BP
Respiratory: Bronchodilation
Therapeutic Uses: In emergencies to stimulate heart rate during bradycardia

11
Q
Dopamine
Classification:
Receptor selectivity:
Cardiovascular (Dose-Dependent):
Therapeutic Uses:
A

Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor selectivity: DA1, β1, α1
Cardiovascular (Dose-Dependent):
- Low dose - vasodilation of renal and mesenteric arteries - decrease peripheral resistance (DA1)
- Medium dose - Increase heart rate, contractile force, cardiac output (β1)
- High dose - Vasoconstriction and increase peripheral resistance (α1)
Therapeutic Uses: Severe decompensated heart failure, shock

12
Q
Dobutamine
Classification:
Receptor Selectivity:
Cardiovascular:
Therapeutic Uses:
A

Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor Selectivity:
-(-) dobutamine - α1 agonist and β agonist
-(+) dobutamine - α1 antagonist and β agonist
Overall effect as β1 agonist
Cardiovascular:
- Increased cardiac rate, contractility and output
- Minimal change in peripheral resistance and blood pressure
Therapeutic Uses: Short term treatment of cardiac decompensation; Cardiac stress testing

13
Q
Methyldopa
Classification:
Receptor Selectivity:
Cardiovascular:
Major Therapeutic Use:
Side Effects:
A

Class: Direct Acting Adrenergic Agonists - Catecholamine
Receptor Selectivity: Stimulate CNS α2 receptors (Inhibit sympathetic outflow)
Cardiovascular: Decreases PVR, HR and CO
Major Therapeutic Use: Anti-hypertensive
Side Effects: Sedation; dry mouth, edema, rebound hypertension

14
Q
Phenylephrine
Classification:
Receptor selectivity:
Cardiovascular:
Therapeutic Use:
A

Class: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: α1 agonist
Cardiovascular: Increases SBP and DBP; Decreases HR (reflex); Decrease blood flow
Therapeutic Use: Nasal decongestant; used with local anesthetics to increase duration of action; treatment of hypotension

15
Q
Clonidine
Classification:
Receptor selectivity:
Cardiovascular:
Therapeutic Use:
A

Classification: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: CNS α2 agonist
Cardiovascular: Prolonged BP lowering, Decrease PVR, HR and CO
Therapeutic Use: Anti-hypertensive agent

16
Q
Albuterol
Classification:
Receptor selectivity:
Therapeutic Use:
Side Effects:
A

Classification: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: Act mainly on β2 adrenergic receptors (short acting)
Therapeutic Use: Bronchodilator
Side Effects: Tremor, anxiety, tachycardia

17
Q
Salmeterol
Classification:
Receptor selectivity:
Therapeutic Use:
Onset:
A

Classification: Direct Acting Adrenergic Agonists - Non-Catecholamine
Receptor selectivity: β2 agonist
Therapeutic Use: Chronic obstructive pulmonary disease, asthma
Onset: Slow onset of action; long duration of action (w/ inhalation)

18
Q
Tyramine:
Classification:
Action:
Metabolized: 
Source:
A

Classification: Indirect acting adrenergic agonist
Action: Releases NE from sympathetic nerves
Metabolized: to inactive products by MAO
Source: High levels in fermented foods

19
Q
Amphetamine
Classification:
Receptor Activation:
Action:
Therapeutic Use:
A

Classification: Mixed acting adrenergic agonist
Receptor Activation: Peripheral α and β receptor actions, and also weak direct α and β agonist
Action: Releases NE from adrenergic neurons; weakly blocks NET; depresses appetite
Therapeutic Use: Narcolepsy; ADD

20
Q
Ephedrine:
Class:
Receptor Activation:
Action:
Therapeutic use:
A

Class: Mixed acting adrenergic agonist
Receptor Activation: α and β receptor direct agonist
Action: Releases NE and CNS stimulation
Therapeutic use: Previously used to treat asthma but has been replaced by β2 agonists

21
Q
Pseudoephedrine
Class:
Receptor Activation:
Action:
Therapeutic use:
A

Class: Mixed acting adrenergic agonist
Receptor Activation: Direct α1 agonist activity with little β2 agonist activity
Action: Orally effective but less CNS stimulation - precursor to Methamphetamine
Therapeutic use: Nasal decongestant

22
Q
Guanethidine/Guanadrel
Class:
Action:
Therapeutic Use:
Side Effects:
A

Class: Adrenergic antagonist (neuron blocker)
Action: Inhibits NE release, and deplete neuronal amine stores - Taken into adrenergic nerves by NET; effects inhibited by tricyclic antidepressants that also inhibit the NET
Therapeutic Use: Orally active compounds used to treat severe hypertension
Side Effects: Numerous, limit use, interferes w/ sexual function

23
Q
Reserpine
Class:
Action:
Therapeutic Use:
Side Effects:
A

Class: Adrenergic antagonist (Neuron blocker)
Action: Diffuses into adrenergic nerves (w/o NET) and depletes neurotransmitters - inhibits VMAT2
Therapeutic Use: Orally active compound used to treat essential hypertension
Side Effects: Depression, suicide, sedation

24
Q
Phenoxybenzamine
Class:
Receptors blocked (mechanism):
Action:
Therapeutic Use:
A

Class: Adrenergic antagonist (Receptor blocker)
Receptors blocked (mechanism): α1 and α2 receptors; irreversible antagonist
Action: Produces vasodilation porportional to degree of sympathetic tone (Long duration of action)
Therapeutic Use: pheochromcytoma

25
Q
Phentolamine:
Class:
Receptors blocked (mechanism):
Action:
Therapeutic Use:
A
Class: Adrenergic antagonist (Receptor blocker)
Receptors blocked (mechanism): α1 and α2 receptors; competitive reversible antagonist
Action: Block can be overcome by increasing levels of agonists (short duration of action)
Therapeutic Use: Hypertension; Pheochromcytoma; Reverses or shortens the duration of soft tissue anesthesia produced by combined local anesthetic and sympathomimetic
26
Q
Prazosin
Class:
Receptors blocked (mechanism):
Action:
Therapeutic Use:
Side effects:
A

Class: Adrenergic antagonist (Receptor blocker)
Receptors blocked (mechanism): α1 (α2); competitive antagonist
Action: Minimal tachycardia; decreases vascular tone in resistance and and capacitance beds; produces less LDL and more HDL
Therapeutic Use: Hypertension; short term congestive heart failure; Benign protostatic hyperplasia
Side Effects: First dose phenomenon - hypotension and syncope 30-90 minutes after first dose

27
Q
Tamsulosin
Class:
Receptors blocked (mechanism):
Action:
Therapeutic Use:
A

Class: Adrenergic antagonist (receptor blocker)
Receptors blocked (mechanism): α1 (with selectivity for α1A receptors over α1B receptors)
Action: Acts on α1 receptors in prostate
Therapeutic Use: Effective treatment for BPH

28
Q
Propanolol
Class:
Receptors blocked (mechanism):
Therapeutic Use:
Side Effects:
A

Class: Adrenergic receptor antagonist (First generation)
Receptors blocked (mechanism): β1 and β2 receptors (Competitive reversible antagonist)
Therapeutic Use: Hypertension; angina; Cardiac arrhythmias due to excess catecholamines; migraine prophylaxis
Side Effects: Cardiac depression, bradycardia/heart block; may increase airway resistance

29
Q

Timolol
Class:
Receptors blocked (mechanism):
Therapeutic Use:

A

Class: Adrenergic Receptor Antagonist (First Generatio)n
Receptors blocked (mechanism): Non selective β
Therapeutic Use: Same as propanolol; also used in treatment of wide angle glaucoma

30
Q

Metoprolol
Class:
Receptors Blocked:
Therapeutic Use:

A

Class: Adrenergic Receptor Antagonist (Second generation)
Receptors Blocked: β1 (Competitive reversible)
Therapeutic Use: Same as propanolol; also used to treat heart failure

31
Q

Atenolol
Class:
Therapeutic Use:
Action:

A

Class: Adrenergic Receptor Antagonist (Second Generation)
Therapeutic Use: Similar to popanolol (except for migrain prophylaxis)
Action: Does not penetrate into CNS – less CNS side effects

32
Q

Labetalol
Class:
Receptors blocked:
Therapeutic Use:

A

Class: Adrenergic Receptor Antagonist (Third Generation)
Receptors blocked: α1 receptor and both β receptors (competitive antagonist)
Therapeutic Use: Essential hypertension (oral) and hypertensive emergencies (IV)

33
Q
Carvedilol
Class:
Receptors blocked:
Actions
Therapeutic Use:
A

Class: Adrenergic Receptor Antagonist (Third Generation)
Receptors blocked: α1 receptor and both β receptors (competitive antagonist)
Actions: Blocks L-type Calcium channels at higher doses
Therapeutic Use: Chronic heart failure, hypertension, and acute MI

34
Q

Acetycholine

A

Choline ester: Opthalmic for rapid miosis

35
Q
Bethanechol
Classification:
Primary Effect:
Therapeutic Uses:
Side Effects:
A

Classification: Muscarinic Agonist - Choline Esters
Primary Effect: G.I/G.U system
Therapeutic Uses: Orally or subcutaneous for urinary retention in the absence of obstruction
SE: SLUDGE, hypotension, bradycardia, blurred vision

36
Q

Muscarine

A

Present in some species of mushrooms

37
Q

Pilocarpine:
Classification:
Therapeutic Uses:
Side Effects:

A

Classification: Muscarinic Agonist - Alkaloid
Therapeutic Uses: Orally for xerostomia
- Miotic agent used opthalmically to treat wide-angle glaucoma as well as emergency treatment for narrow angle glaucoma
SE: SLUDGE, hypotension, bradycardia, blurred vision

38
Q
Edrophonium
Classification:
Administration:
Therapeutic Use:
Side Effects:
A

Classification:Reversible Acetylcholinesterase Inhibitor
Administration: IV
Therapeutic Use: Diagnosis of myasthenia gravis
- Distinguish cholinergic from myasthenic crisis
- Reverse paralysis by competitive neuromuscular blocking agents
SE: SLUDGE, hypotension, bradycardia, blurred vision

39
Q

Physostigmine
Class:
Therapeutic Use:
Side Effects:

A

Class: Reversible Acetylcholinesterase Inhibitor
Therapeutic Use: Treatment of chronic wide-angle glaucoma
- Toxicity by antimuscarinic drug poisoning - penetrates CNS
SE: SLUDGE, hypotension, bradycardia, blurred vision

40
Q

Neostigmine
Class:
Therapeutic Use:
Side Effects:

A

Class: Reversible Acetylcholinesterase Inhibitor
Therapeutic Use: Treatment of myasthenia gravis (oral)
- Prevention and treatment of post-operative atony of gut and bladder
- Reversal of paralysis by neuromuscular junction blocking agents
SE: SLUDGE, hypotension, bradycardia, blurred vision

41
Q

Nerve Gas
Class:
Toxicity:

A

Sarin
Class: Organophosphate
Toxicity: SLUDGE, medullary respiratory center depression, muscle paralysis due to depolarizing neuromuscular junction blockade

42
Q

Insecticide
Class:
Toxicity:

A

Malathion - Detoxified in humans
Class: Organophosphate
Toxicity: SLUDGE, medullary respiratory center depression, muscle paralysis due to depolarizing neuromuscular junction blockade

43
Q

Atropine
Class:
Therapeutic Use:

A

Class: Muscarinic receptor antagonist - Alkaloid
Therapeutic Use: Bradyarrhythmias
- Opthalmic uses: mydriasis and cycloplegia
- Blocks vagal reflexes and secretions during anesthesia
- Acetylcholinesterase and muscarinic toxicity

44
Q

Pralidoxime

Therapeutic Use:

A

Therapeutic Use: Reactivates Ach peripherally (2-3 hours)

45
Q

Scopolamine
Classification:
Therapeutic Uses:

A

Classification: Muscarinic Receptor Antagonist - Alkaloid

Therapeutic Uses: Motion sickness and vestibular diseases (penetrates CNS)

46
Q

Ipratropium
Class:
Therapeutic Uses:

A

Class: Muscarinic Receptor Antagonists - Semi-synthetic derivatives
Therapeutic Use: COPD (less effective for asthma)

47
Q

Tropicamide
Class:
Therapeutic Use:

A

Class: Muscarinic Receptor Antagonists

Therapeutic Use: Mydriatic and cycloplegic

48
Q

Oxybutynin
Class:
Therapeutic Use:
Side Effects:

A

Class: Muscarinic Receptor Antagonist
Therapeutic Use: Overactive bladder, incontinence
SE: xerostomia, blurred vision, constipation, drowsiness

49
Q

Darifenacin
Class:
Therapeutic Use:

A

Class: Muscarinic Receptor Antagonist

Therapeutic Use: Overactive bladder, incontinence

50
Q

Glycopyrrolate
Class:
Therapeutic:

A

Class: Muscarinic Receptor Antagonist
Therapeutic Use: Used to block parasympathetic effects when neostigmine is used to reverse skeletal muscle paralysis by neuromuscular blocking agents

51
Q

Muscarinic Receptor Antagonist: Side Effects

A
Hot as hare
Dry as bone
Red as a beet
Blind as a bat
Drowsiness
Mad as a hatter
52
Q
Rocuronium
Class:
Duration of Action:
Elimination:
CV effects:
Histamine release:
A

Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Intermediate (30-60 minutes)
Elimination: Liver metabolism
CV effects: Minimal
Histamine release: None

53
Q
Atracurium
Class:
Duration of Action:
Elimination:
CV effects:
Histamine release:
A

Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Intermediate (30-60 minutes)
Elimination: Spontaneously degrades in plasma
CV effects: Minimal
Histamine release: Slight

54
Q
Vercuronium
Class:
Duration of Action:
Elimination:
CV effects:
Histamine release:
A

Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Intermediate (60-90 minutes)
Elimination: Liver metabolism
CV effects: Minimal
Histamine release: None

55
Q
Pancuronium
Class:
Duration of Action:
Elimination:
CV effects:
Histamine release:
A

Class: Competitive Neuromuscular Blocking Agents
Duration of Action: Long (120-180 minutes)
Elimination: Renal excretion
CV effects: Slight increase in HR and BP
Histamine release: Slight

56
Q

Succinylcholine
Class:
Theraputic use:
Metabolized by:

A

Class: Depolarizing Neuromuscular Blocking
Therapeutic Use: Produces muscle fasciculations and then paralysis
Metabolized by: Pseudocholinesteraese