Drugs to Know Flashcards
(40 cards)
Phenobarbital
Class
Clinical Use
Mechanism
Barbituate
Intravenous anesthesia and treatment of epileptic seizures
Binds toGABAA-R receptors ->potentiatesANDdirectly activatesGABAA-R receptors -> neuronal inhibition ->sedation, hypnosis, anterograde amnesia, muscle relaxation
Alprazolam
Class
Clinical Use
Mechanism
Benzodiazepine
Treatment of anxiety disorders, withdrawal, epilepsy, and insomnia
Binds toGABAA-R receptors ->potentiatesGABAA-R receptor action -> neuronal inhibition -> sedation, hypnosis, anterograde amnesia, muscle relaxation
Diazepam
Class
Clinical Use
Mechanism
Benzodiazepine
Treatment of anxiety disorders, withdrawal, epilepsy, and insomnia
Binds toGABAA-R receptors ->potentiatesGABAA-R receptor action -> neuronal inhibition -> sedation, hypnosis, anterograde amnesia, muscle relaxation
Flumazenil
Class
Clinical Use
Mechanism
Benzodiazepine antidote
Counteracts the sedative/hypnotic effects of benzodiazepines
Competitively inhibitsGABAA-R receptors -> relief of neuronal inhibition
Alpha-methyltyrosine
Class
Clinical Use
Mechanism
Indirect sympatholytic
Treatment of pheochromocytoma
Inhibits tyrosine hydroxylase (tyrosine -> DOPA) -> inhibits catecholamine synthesis -> inhibits adrenergic stimulation
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
Reserpine
Class
Clinical Use
Mechanism
Indirect sympatholytic
Antihypertensive
InhibitsVMAT2-> inhibition of vesicular storage of norepinephrine and dopamine -> destruction of norepinephrine and dopamine byMAO->depletionof norepinephrine and dopamine nerve terminals
Amphetamine
Class
Clinical Use
Mechanism
Indirect sympathomimetic
Treatment of ADHD
Causes pre-synaptic release of norepinephrine from the mobile pool -> indirect adrenergic stimulation
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
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)”
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”
Lidocaine
Class
Clinical Use
Mechanism
Local anesthetic (amide)
Local anesthesia
Inhibits voltage-gated Na+channels -> prevents membrane depolarization and action potential generation -> neuronal inhibition
Pilocarpine
Class
Clinical Use
Mechanism
MAchR agonist
Treatment of glaucoma, xerostemia; diagnosis of cystic fibrosis
Activation of MAchR -> increased vagal tone
Dopamine
Class
Clinical Use
Mechanism
Mixed adrenergic agonist
Treatment of decompensated congestive heart failure (with medium doses -> β1)
D > β1>α
Epinephrine
Class
Clinical Use
Mechanism
Mixed adrenergic agonist
Treatment of cardiac arrest, cardiogenic shock, severe hypotension, anaphylaxis and asthma
β2>β1>α1>α2
Norepinephrine
Class
Clinical Use
Mechanism
Mixed adrenergic agonist
Treatment of cardiac arrest, cardiogenic shock, and severe hypotension
β1≥α1>α2
Phenylephrine
Class
Clinical Use
Mechanism
α1 agonist
Nasal decongestant and dilation of pupils
Activation of α1 receptors -> smooth muscle contraction -> vasoconstriction (nasal decongestion) + mydriasis
Clonidine
Class
Clinical Use
Mechanism
α2 agonist
Treatment of hypertension
Activation of presynapticα2receptors -> decreased sympathetic outflow -> decreased blood pressure
Phenoxybenzamine
Class
Clinical Use
Mechanism
α antagonist (nonspecific)
Treatment of hypertension (especially in patients with pheochromocytoma)
Irreversibly inhibitsα1andα2receptors-> dilation of vascular smooth muscle -> decreased blood pressure
Phentolamine
Class
Clinical Use
Mechanism
α antagonist (nonspecific)
Treatment of hypertension (especially in patients with pheochromocytoma)
Reversibly inhibitsα1andα2receptors-> dilation of vascular smooth muscle -> decreased blood pressure
Doxazosin
Class
Clinical Use
Mechanism
α1 antagonist
Treatment of hypertension and benign prostatic hyperplasia
α1-receptor blockade -> vasodilation -> decreased blood pressure
Isoproterenol
Class
Clinical Use
Mechanism
β agonist (nonspecific)
Treatment of bradycardia, heart block, and bronchospasm
“Activation ofβ1receptors -> increased heart rate, contractility, conductivity
Activation ofβ2receptors -> bronchodilation”
Dobutamine
Class
Clinical Use
Mechanism
β1 agonist
Treatment of decompensated congestive heart failure
β1 receptor activation -> increased heart rate, contractility, conductivity
Albuterol
Class
Clinical Use
Mechanism
β2 agonist
Relief of asthma-related bronchospasm
β2 receptor activation -> relaxation of smooth muscle -> bronchodilation