Drugs to Know Flashcards Preview

Pharmacology > Drugs to Know > Flashcards

Flashcards in Drugs to Know Deck (40):
1

Phenobarbital

Class

Clinical Use

Mechanism

Barbituate

Intravenous anesthesia and treatment of epileptic seizures

Binds to GABAA-R receptors -> potentiates AND directly activates GABAA-R receptors -> neuronal inhibition -> sedation, hypnosis, anterograde amnesia, muscle relaxation

2

Alprazolam

Class

Clinical Use

Mechanism

Benzodiazepine

Treatment of anxiety disorders, withdrawal, epilepsy, and insomnia

Binds to GABAA-R receptors -> potentiates GABAA-R receptor action -> neuronal inhibition -> sedation, hypnosis, anterograde amnesia, muscle relaxation

3

Diazepam

Class

Clinical Use

Mechanism

Benzodiazepine

Treatment of anxiety disorders, withdrawal, epilepsy, and insomnia

Binds to GABAA-R receptors -> potentiates GABAA-R receptor action -> neuronal inhibition -> sedation, hypnosis, anterograde amnesia, muscle relaxation

4

Flumazenil

Class

Clinical Use

Mechanism

Benzodiazepine antidote

Counteracts the sedative/hypnotic effects of benzodiazepines

Competitively inhibits GABAA-R receptors -> relief of neuronal inhibition

5

Alpha-methyltyrosine

Class

Clinical Use

Mechanism

Indirect sympatholytic

Treatment of pheochromocytoma

Inhibits tyrosine hydroxylase (tyrosine -> DOPA) -> inhibits catecholamine synthesis -> inhibits adrenergic stimulation

6

Guanethidine

Class

Clinical Use

Mechanism

Indirect sympatholytic

Treatment of hypertension, especially during pregnancy

Inhibits pre-synaptic release of norepinephrine from storage vesicles -> inhibits adrenergic stimulation

7

Reserpine

Class

Clinical Use

Mechanism

Indirect sympatholytic

Antihypertensive

Inhibits VMAT2 -> inhibition of vesicular storage of norepinephrine and dopamine -> destruction of norepinephrine and dopamine by MAO -> depletion of norepinephrine and dopamine nerve terminals

8

Amphetamine

Class

Clinical Use

Mechanism

Indirect sympathomimetic

Treatment of ADHD

Causes pre-synaptic release of norepinephrine from the mobile pool -> indirect adrenergic stimulation

9

Tyramine

Class

Clinical Use

Mechanism

Indirect sympathomimetic

Induce fat loss, increase glucose uptake, affects blood pressure

Causes pre-synaptic release of norepinephrine from the mobile pool -> indirect adrenergic stimulation

10

Ephedrine

Class

Clinical Use

Mechanism

Indirect sympathomimetic*

Nasal decongestant

"1) Causes pre-synaptic release of norepinephrine from the mobile pool -> indirect adrenergic stimulation (strong)
2) Directly activates post-synaptic adrenergic receptors (weak)"

11

Cocaine

Class

Clinical Use

Mechanism

Indirect sympathomimetic

Local anesthesia + local vasoconstriction

"1) Inhibits uptake-1 (neuronal) of norepinephrine -> synaptic accumulation of NE -> indirect adrenergic stimulation
2) Inhibits voltage-gated Na+ channels -> prevents membrane depolarization and action potential generation -> neuronal inhibition"

12

Lidocaine

Class

Clinical Use

Mechanism

Local anesthetic (amide)

Local anesthesia

Inhibits voltage-gated Na+ channels -> prevents membrane depolarization and action potential generation -> neuronal inhibition

13

Pilocarpine

Class

Clinical Use

Mechanism

MAchR agonist

Treatment of glaucoma, xerostemia; diagnosis of cystic fibrosis

Activation of MAchR -> increased vagal tone

14

Dopamine

Class

Clinical Use

Mechanism

Mixed adrenergic agonist

Treatment of decompensated congestive heart failure (with medium doses -> β1)

D > β1 > α

15

Epinephrine

Class

Clinical Use

Mechanism

Mixed adrenergic agonist

Treatment of cardiac arrest, cardiogenic shock, severe hypotension, anaphylaxis and asthma

β2 > β1 > α1 > α2

16

Norepinephrine

Class

Clinical Use

Mechanism

Mixed adrenergic agonist

Treatment of cardiac arrest, cardiogenic shock, and severe hypotension

β1 ≥ α1 > α2

17

Phenylephrine

Class

Clinical Use

Mechanism

α1 agonist

Nasal decongestant and dilation of pupils

Activation of α1 receptors -> smooth muscle contraction -> vasoconstriction (nasal decongestion) + mydriasis

18

Clonidine

Class

Clinical Use

Mechanism

α2 agonist

Treatment of hypertension

Activation of presynaptic α2 receptors -> decreased sympathetic outflow -> decreased blood pressure

19

Phenoxybenzamine

Class

Clinical Use

Mechanism

α antagonist (nonspecific)

Treatment of hypertension (especially in patients with pheochromocytoma)

Irreversibly inhibits α1 and α2 receptors -> dilation of vascular smooth muscle -> decreased blood pressure

20

Phentolamine

Class

Clinical Use

Mechanism

α antagonist (nonspecific)

Treatment of hypertension (especially in patients with pheochromocytoma)

Reversibly inhibits α1 and α2 receptors -> dilation of vascular smooth muscle -> decreased blood pressure

21

Doxazosin

Class

Clinical Use

Mechanism

α1 antagonist

Treatment of hypertension and benign prostatic hyperplasia

α1-receptor blockade -> vasodilation -> decreased blood pressure

22

Isoproterenol

Class

Clinical Use

Mechanism

β agonist (nonspecific)

Treatment of bradycardia, heart block, and bronchospasm

"Activation of β1 receptors -> increased heart rate, contractility, conductivity
Activation of β2 receptors -> bronchodilation"

23

Dobutamine

Class

Clinical Use

Mechanism

β1 agonist

Treatment of decompensated congestive heart failure

β1 receptor activation -> increased heart rate, contractility, conductivity

24

Albuterol

Class

Clinical Use

Mechanism

β2 agonist

Relief of asthma-related bronchospasm

β2 receptor activation -> relaxation of smooth muscle -> bronchodilation

25

Terbutaline

Class

Clinical Use

Mechanism

β2 agonist

Relief of asthma-related bronchospasm

β2 receptor activation -> relaxation of smooth muscle -> bronchodilation

26

Propanolol

Class

Clinical Use

Mechanism

β antagonist (nonspecific)

Treatment of ischemic heart disease, hypertension, and tachyarrhythmias

"β1-receptor blockade -> decreased heart rate, conductivity, and contractility
β2-receptor blockade -> vasoconstriction"

27

Metoprolol

Class

Clinical Use

Mechanism

β1 antagonist

Treatment of ischemic heart disease, hypertension, and tachyarrhythmias

β1-receptor blockade -> decreased heart rate, conductivity, and contractility

28

Esmolol

Class

Clinical Use

Mechanism

β1 antagonist

Treatment of ischemic heart disease, hypertension, and tachyarrhythmias (shorter acting than metoprolol)

β1-receptor blockade -> decreased heart rate, conductivity, and contractility

29

ACE (angiotensin converting enzyme) inhibitors

Class

Clinical Use

Mechanism

Inhibitor of renin-angiotensin system

Treat hypertension

Block the angiotensin converting enzyme (ACE), inhibit the conversion of angiotensin I to angiotensin II -> vasoconstriction, reduced BP

30

Acetaminophen

Class

Clinical Use

Mechanism

Analgesic, Antipyretic

Treat mild to moderate pain, reduce fever

Acts primarily in CNS, increases pain threshold by indirectly inhibiting cyclooxygenase in prostaglandin synthesis

31

ADH (anti-diuretic hormone, aka vasopressin)

Class

Clinical Use

Mechanism

Posterior Pituitary Hormone

Prevents water loss in the kidney, restores BP in hypovolemic shock

Released by posterior pituitary when water deprivation causes increased plasma osmolarity or when cardiovascular system is challenged by hypovolemia and/or hypotension, increases peripheral vascular resistance (vasoconstriction) and increases arterial blood pressure, promotes release of coagulation factors by vascular endothelium, increases platelet aggregability

32

Aldosterone

Class

Clinical Use

Mechanism

Steroid Hormone (Mineralocorticoid)

Increases systemic blood pressure, augments potassium and hydrogen excretion

Acts on distal tubules and collecting ducts of nephron, increases sodium & water reabsorption

33

Angiotensin II

Class

Clinical Use

Mechanism

Vasoactive octapeptide produced by angiotensin I

Stimulates vascular smooth muscle, promotes aldosterone produciton, stimulates SNS

Inhibits renin release

34

Bradykinin

Class

Clinical Use

Mechanism

Kinin, acts on bradykinin receptors B1 and B2 (GPCRs)

Treats hypertension (vasodilator), contracts non-vascular smooth muscle in the bronchus & gut, increases vascular permeability, causes natriuresis

Raises internal Ca levels, causes neocortical astrocytes to release glutamate; also converted bo inactive metabolites by ACE, so ACEIs increase levels, cause bronchoconstriction

35

Desipramine

Class

Clinical Use

Mechanism

Tricyclic Antidepressant (TCA)

Treats depression, neuropathic pain, ADHD, & cocaine withdrawal

Inhibits reuptake of NE (& SE)

36

Enalapril

Class

Clinical Use

Mechanism

ACEI

Treats hypertension, diabetic nephropathy, & some types of chronic heart failure

Prevents conversion of ang I to ang II, inhibits vasoconstricting effects of ang II, decreases BP

37

Histamine

Class

Clinical Use

Mechanism

Targets histamine receptors (GPCRs)

Involved in local immune responses and inflammatory responses, stimulates gastric secretion, constricts bronchial smooth muscle, vasodilator, treats hypertension

Acts directly on blood vessels to dilate arteries & capilaries via histamine receptors

38

Nicotine

Class

Clinical Use

Mechanism

Nicotinic acetylcholine receptor agonist

Treats nicotine dependence

Enters body, quickly distributed through bloodstream, crosses BBB, metabolized in liver

39

Phenytoin

Class

Clinical Use

Mechanism

Antiepileptic drug

Treats seizures

Binds to inactive form of sodium channels, blocks sodium-dependent action potentials

40

Renin

Class

Clinical Use

Mechanism

Renin-Angiotensin System Enzyme

Activates the renin-angiotensin system, increases BP to restore perfusion pressure in kidneys

Renin cleaves angiotensinogen -> ang I, ACE converts ang I -> ang II, ang Ii constricts blood vessels, increases secretion of ADH & aldosterone, & stimulates hypothalamus to activate thirs treflex, results in increased blood pressure