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Pharm CH 09
Adrenoceptor Agonists & Sympathomimetic Drugs
16
Pharmacology
Professional
05/27/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Epinephrine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Endogenous Catecholamine

 

Agonist of α and β receptors; positive ionotropic (contractility) and chronotropic (rate) on heart (β1), vasoconstriction in vascular beds (α), and vasodilation in skeletal muscle blood vessels (β2) which may lower TPR

tachycardia, arrhythmia, anxiety, hypertension, and acute pulmonary edema

Cardiac arrest (increases cardiac output), anaphylaxis

 

Term
Norepinephrine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Endogenous catecholamine

 

Agonist of α1, α2, and β1 receptors but little effect on β2; increases TPR and BP, positive ionotropic effect on heart

Ischemia, arrhythmias

Hypotension, ADHD, depression

 

Term
Dopamine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Endogenous Catecholamine

 

Activates D1 receptors causing vasodilation of renal, splanchnic, coronary, cerebral, and other resistance vessels. Activation of D2 receptors suppresses norepinephrine release. Also activates β1receptors in heart and at high concentrations α receptors leading to vasoconstriction. Regulates Na+ secretion and renal function.  Neurotransmitter in the CNS and is involved in reward system of addiction.

Hypotension at high doses

Parkinson’s disease (caused by a deficiency of dopamine in basal ganglia); Dopamine receptors are targets for antipsychotic drugs

 

Term
Phenylephrine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Direct-Acting Sympathomimetic

 

α1 agonist; vasoconstriction = ↑ arterial resistance and ↓ venous capacity, ↑ stroke volume causes ↑ CO, ↑ BP may cause reflexive ↓ HR; α1 r’s also constrict pupillary dilator muscle

hypertension

Decongestant, mydriatic (dilates pupil), can be used to increase BP

 

Term
Clonidine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Direct-Acting Sympathomimetic

 

α2 agonist; cause vasoconstriction when given locally, but systemically acts through CNS to decrease sympathetic tone and BP

Dry mouth, sedation

Drowsiness

Impaired ejaculation

hypertension

 

Term
Oxymetazoline
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Direct-Acting Sympathomimetic

 

α agonist with affinity for α2A receptor; promotes vasoconstriction of nasal mucosa

Hypotension (central Clonidine-like effect)

Topical decongestant

 

Term
Isoproterenol
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Direct-Acting Sympathomimetic

 

Potent β1 and β2 agonist, positive chronotropic and ionotropic effects, vasodilator = ↑ CO, ↓ TPR and ↓ BP

Tachycardia, dysrhythmias

Bradycardia, heart block

 

Term
Dobutamine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Direct-Acting Sympathomimetic

 

Β1 agonist; activate β1 receptors causing ↑ CO with less reflexive tachycardia because they do not activate vasodilator β2 receptors

Hypertension, arrhythmias

Heart failure, cardiogenic shock

 

Term
Ephedrine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Mixed-Acting Sympathomimetic

 

Indirect stimulation of the adrenergic receptor system by increasing the activity of noradrenaline at α- and β-receptors, ability to cross blood-brain barrier into CNS makes it a mild stimulant

Tachycardia, arrhythmias, various nervous system symptoms

Ma huang (herbal medicine) decongestant, bronchodilator, weight loss

 

Term
Amphetamine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Indirect-Acting Sympathomimetics

 

Acts as both a norepinephrine transporter (NET) substrate and reuptake blocker, eliciting reverse transport and blocking normal uptake = ↑ NE in synaptic cleft; release of NE and some dopamine; similar to ephedrine but enters CNS more readily

Elevates CO and BP

CNS stimulation

Marked stimulant effect on mood and alertness and depressant effect on appetite

 

Term
Methylphenidate
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Indirect-Acting Sympathomimetics

 

Pharmacologic effects and abuse potential are similar to amphetamine (p.141); Block NET-mediated NE reuptake and enhance NE signaling similar to cocaine (p. 133) ???

Nervousness, drowsiness, insomnia

ADHD, narcolepsy

 

Term
Modafinil
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Indirect-Acting Sympathomimetics

 

Inhibits both norepinephrine and dopamine transporters; increases interstitial concentrations not only of norepinephrine, dopamine, serotonin, and glutamate; decreases GABA levels

Increase in BP and HR

Improves wakefulness in narcolepsy and some other conditions

 

Term
Tyramine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Indirect-Acting Sympathomimetics

 

Indirect sympathomimetic action caused by release of stored catecholamines = action similar to NE; readily metabolized by MAO in liver = high first-pass effect

Increase in BP

Hypertensive crisis

Patients treated with monoamine oxidase (MAO) inhibitors may have intensified Tyramine effect (must avoid Tyramine containing foods like cheese)

 

Term
Cocaine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Catecholamine Reuptake Inhibitor

 

Inhibits transmitter reuptake at noradrenergic synapses; enters CNS and inhibits dopamine reuptake into neurons in the “pleasure centers” of the brain

Tachycardia, hallucinations, paranoid delusions; overdoses cause tachyarrhythmias and a marked ↑ BP, which can be life-threatening. CNS stimulation

Heavily abused drug - produces amphetamine-like”psychological effects that is shorter lasting and more intense

 

Term
Fenoldopam
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Dopamine Agonist

 

D1 agonist; activates adenylyl cyclase; causes vascular smooth muscle relaxation

hypotension, reflex tachycardia, ↑ intraocular pressure

hypertension

 

Term
Bromocryptine
Definition

CH 9 Adrenoceptor Agonists & Sympathomimetic Drugs

Dopamine Agonist

 

D2 agonists; inhibits adenylyl cyclase and interacts with other intracellular pathways; restores dopamine actions in the CNS

Orthostatic hypotension

Parkinson’s disease, prolactinemia

 

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