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Adrenergric Pharmacology
Drugs
34
Biology
Graduate
03/15/2012

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Term
Metyrosine
Definition
Inhibits Tyrosine hydroxylase
Used to treat pheochromocytoma
Term
Carbidopa
Definition
Inhibits AAAd (DOPA decarboxylase)
Used to treat Parkinson's
Does not cross the blood brain barrier
Term
Deprenyl
Definition
Inhibits Monoamine Oxidase-B
Used to treat Parkinson's
Term
Disulfiram
Definition
Inhibits Dopamine β-hydroxylase, DBH
(Cu-chelator) is used to treat alcoholism
Term
Reserpine
Definition
Mechanism: Permanently inhibits amine-H+ exchanger in vesicular membranes needed for catecholamine packaging, can cross the BBB
End Effect: Depletes catecholamine stores

Use: Hypertension, psychosis

SE: Depression, GI hemorrhage, diarrhea, nasal stuffiness

Note: “Hit and run”, action of drug much longer than plasma half-life
Term
Clonidine
Definition
Mechanism: α2 receptor agonist, inhibits release of catecholamine-containing vesicles in the CNS
End Effect: Reduces catecholamines in the synapse

Use: Hypertension therapy (w/ renal issues due to CNS action),
SE: Dry mouth, somnolence,
Term
Guanethidine/Guanadrel
Definition
Mechanism: 1) Blocks release of packaged catecholamines, 2) requires Uptake 1 to enter nerve terminal and inhibits it based on competition, does not cross the BBB
End Effect: Depletes catecholamine stores

Use: Hypertension

SE: Postural hypotension
Term
Tyramine
Definition
Mechanism: 1) Displaces catecholamines out of the nerve terminal, 2) requires Uptake 1 to enter nerve terminal and inhibits it
End Effect: Increases catecholamines in the synapse

SE w/ MAOIs: Hypertensive crisis, “Cheese Syndrome”

Note: Found in some wine, cheeses, pickled meats, chocolates, alcoholic beverages, fruits, and vegetables

Usually metabolized by monoamine oxidase (MAO), but with MAO-inhibitors on board, tyramine exerts its effect

Requires Uptake-1 to get into the nerve terminal and inhibits competitively. If Uptake-1 is inhibited by another agent, it cannot exert its effect.
Term
Amphetamines/Ephedrine
Definition
Mechanism: 1) Displaces catecholamines out of the nerve terminal, 2) requires Uptake 1 to enter nerve terminal and inhibits
End Effect: Increases catecholamines in the synapse

Amphetamine Use: Stimulant, drug of abuse (hyperactivity, dilated pupils, dry mouth, erectile dysfunction, tachycardia, increased breathing rate, increased blood pressure, fever, sweating, insomnia, and arrhythmia)

Ephedrine Use: Stimulant, decongestant, appetite suppressant, increase wakefulness
Term
Tricyclic Anti-Depressants
Definition
Mechanism: Inhibits Uptake 1, cross BBB acts on CNS mainly

End Effect: Increases catecholamines in the synapse
Use: Depression,
SE: sudden death

Note: Examples of TCAs include desipramine, imipramine, amitriptyline
Term
Cocaine
Definition
Mechanism: CNS: Inhibits Uptake 1, Peripheral: Inhibits Na+ channel
End Effect: Increases catecholamines in the synapse; prevents neuronal excitation
Use: Local anesthetic, recreational drug (euphoria, increased heart rate, increased blood pressure)
Term
α1
Definition
↑ BP
Term
α2
Definition
decrease BP (pre-synaptic)
Term
β1
Definition
↑ HR, cardiac contractility
Term
β2
Definition
Bronchodilation, decrease BP
Term
Epinephrine (Adrenaline)
Definition
Mechanism: α1, α2, β1, β2 agonist
Use: Cardiac arrest, ↑ low cardiac output, anaphylaxis (↓ BP, cardiac output), added to local anesthetics, among other uses

Notes: Action is evenly split between α and β receptor agonism
Term
Norepinephrine (Noradrenaline)
Definition
Mechanism: α1, α2, β1 agonist
Use: Hypotension in the critical care setting

Notes: Predominantly stimulates α receptors with relatively little β1 stimulation
Term
Phenylephrine
Definition
Mechanism: α1 agonist
Use (SE): Decongestant, pupil dilator, septic shock, and profound hypotension
Term
methoxamine
Definition
Mechanism: α1 agonist
Use (SE): Decongestant, pupil dilator, septic shock, and profound hypotension
Term
Clonidine
Definition
Mechanism: α2 agonist
Use (SE): Treatment for hypertension
Term
α-methylnoradrenaline
Definition
Mechanism: α2 agonist
Use (SE): Treatment for hypertension
Term
Phenoxybenzamine
Definition
Mechanism: α1, 2 antagonist
Use: pheochromocytoma (phenoxybenzamine)
Term
phentolamine
Definition
Mechanism: α1, 2 antagonist
Use: pheochromocytoma (phenoxybenzamine)
Term
Prazosin
Definition
Mechanism: α1 antagonist
Use: Treatment for hypertension
Term
Yohimbine
Definition
Mechanism: α2 antagonist
Use: None
Term
Isoproterenol
Definition
Mechanism: β1, 2 agonist
Term
Dobutamine
Definition
Mechanism: β1 agonist
Use: Stress test, heart failure, shock
Term
Albuterol
Definition
Mechanism: β2 agonist
Use: Asthma, pre-term labor (tocolytic)
Term
terbutaline
Definition
Mechanism: β2 agonist
Use: Asthma, pre-term labor (tocolytic)
Term
Propranolol
Definition
Mechanism: β1, 2 antagonist
Use: Hypertension, migraine prophylaxis
Term
Atenolol
Definition
Mechanism: β1 antagonist
Use: Hypertension, arrhythmia, angina, myocardial infarction
Term
metoprolol
Definition
Mechanism: β1 antagonist
Use: Hypertension, arrhythmia, angina, myocardial infarction
Term
Carvedilol
Definition
Mechanism: α1, β1, 2 antagonist
Use: Heart Failure
Term
Nebivolol
Definition
Mechanism: β1 antagonist + vasodilation (NO-like)
Use: Hypertension, Heart Failure
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