Drugs Flashcards

(56 cards)

1
Q

Isoniazid

A

Anti-tuberculosis drug metabolized by N-acetyltransferase-2

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2
Q

Anti-depressants

A

Metabolized by CYP2D6

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3
Q

Omeprazole, Phenytoin, Clopidogrel

A

Metabolized by CYP2C19

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4
Q

Warfarin

A

Metabolized by CYP2C9

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

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5
Q

Succinylcholine

A

a depolarizing muscle relaxant - treatment affected by pseudocholinesterase polymorphism

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6
Q

Mercaptopurine

A

Bone marrow suppression in cancer treatment

- treatment affected by TPMPT polymorphism

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7
Q

Digoxin

A

Cardiac glycoside - Treatment affected by P-glycoprotein polymorphism

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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

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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

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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

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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

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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

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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

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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

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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

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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

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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)

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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

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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

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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

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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

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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

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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
``` Phentolamine: Class: Receptors blocked (mechanism): Action: Therapeutic Use: ```
``` 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
``` Prazosin Class: Receptors blocked (mechanism): Action: Therapeutic Use: Side effects: ```
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
``` Tamsulosin Class: Receptors blocked (mechanism): Action: Therapeutic Use: ```
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
``` Propanolol Class: Receptors blocked (mechanism): Therapeutic Use: Side Effects: ```
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
Timolol Class: Receptors blocked (mechanism): Therapeutic Use:
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
Metoprolol Class: Receptors Blocked: Therapeutic Use:
Class: Adrenergic Receptor Antagonist (Second generation) Receptors Blocked: β1 (Competitive reversible) Therapeutic Use: Same as propanolol; also used to treat heart failure
31
Atenolol Class: Therapeutic Use: Action:
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
Labetalol Class: Receptors blocked: Therapeutic Use:
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
``` Carvedilol Class: Receptors blocked: Actions Therapeutic Use: ```
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
Acetycholine
Choline ester: Opthalmic for rapid miosis
35
``` Bethanechol Classification: Primary Effect: Therapeutic Uses: Side Effects: ```
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
Muscarine
Present in some species of mushrooms
37
Pilocarpine: Classification: Therapeutic Uses: Side Effects:
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
``` Edrophonium Classification: Administration: Therapeutic Use: Side Effects: ```
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
Physostigmine Class: Therapeutic Use: Side Effects:
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
Neostigmine Class: Therapeutic Use: Side Effects:
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
Nerve Gas Class: Toxicity:
Sarin Class: Organophosphate Toxicity: SLUDGE, medullary respiratory center depression, muscle paralysis due to depolarizing neuromuscular junction blockade
42
Insecticide Class: Toxicity:
Malathion - Detoxified in humans Class: Organophosphate Toxicity: SLUDGE, medullary respiratory center depression, muscle paralysis due to depolarizing neuromuscular junction blockade
43
Atropine Class: Therapeutic Use:
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
Pralidoxime | Therapeutic Use:
Therapeutic Use: Reactivates Ach peripherally (2-3 hours)
45
Scopolamine Classification: Therapeutic Uses:
Classification: Muscarinic Receptor Antagonist - Alkaloid | Therapeutic Uses: Motion sickness and vestibular diseases (penetrates CNS)
46
Ipratropium Class: Therapeutic Uses:
Class: Muscarinic Receptor Antagonists - Semi-synthetic derivatives Therapeutic Use: COPD (less effective for asthma)
47
Tropicamide Class: Therapeutic Use:
Class: Muscarinic Receptor Antagonists | Therapeutic Use: Mydriatic and cycloplegic
48
Oxybutynin Class: Therapeutic Use: Side Effects:
Class: Muscarinic Receptor Antagonist Therapeutic Use: Overactive bladder, incontinence SE: xerostomia, blurred vision, constipation, drowsiness
49
Darifenacin Class: Therapeutic Use:
Class: Muscarinic Receptor Antagonist | Therapeutic Use: Overactive bladder, incontinence
50
Glycopyrrolate Class: Therapeutic:
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
Muscarinic Receptor Antagonist: Side Effects
``` Hot as hare Dry as bone Red as a beet Blind as a bat Drowsiness Mad as a hatter ```
52
``` Rocuronium Class: Duration of Action: Elimination: CV effects: Histamine release: ```
Class: Competitive Neuromuscular Blocking Agents Duration of Action: Intermediate (30-60 minutes) Elimination: Liver metabolism CV effects: Minimal Histamine release: None
53
``` Atracurium Class: Duration of Action: Elimination: CV effects: Histamine release: ```
Class: Competitive Neuromuscular Blocking Agents Duration of Action: Intermediate (30-60 minutes) Elimination: Spontaneously degrades in plasma CV effects: Minimal Histamine release: Slight
54
``` Vercuronium Class: Duration of Action: Elimination: CV effects: Histamine release: ```
Class: Competitive Neuromuscular Blocking Agents Duration of Action: Intermediate (60-90 minutes) Elimination: Liver metabolism CV effects: Minimal Histamine release: None
55
``` Pancuronium Class: Duration of Action: Elimination: CV effects: Histamine release: ```
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
Succinylcholine Class: Theraputic use: Metabolized by:
Class: Depolarizing Neuromuscular Blocking Therapeutic Use: Produces muscle fasciculations and then paralysis Metabolized by: Pseudocholinesteraese