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