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46 Cards in this Set
- Front
- Back
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Alpha 1
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Location: Postsynaptic effector cells (esp. vascular SM)
Receptor Signaling: Formation of IP3 & DAG, increased intracellular Ca |
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Alpha 2
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Location: Presynaptic adrenergic nerve terminals, platelets, lipocytes, SM
Receptor Signaling: Inhibition of adenylate cyclase, decreased cAMP |
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Beta 1
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Location:
1) Postsynaptic effector cells (esp. heart, lipocytes, brain) 2) Presynaptic adrenergic & cholinergic nerve terminals, JG apparatus of renal tubules, ciliary body epithelium Receptor Signaling: Stimulation of adenylate cyclase, increased cAMP |
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Beta 2
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Location: Postsynaptic effector cells (esp. SM, respiratory, vascular, uterine, & cardiac muscle)
Receptor Signaling: Stimulation of adenylate cyclase, increased cAMP. Activates cardiac ___ under some conditions |
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Beta 3
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Location: Postsynaptic effector cells (esp. lipocytes)
Receptor Signaling: Stimulation of adenylate cyclase, increased cAMP |
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D 1
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Location: Brain, effector tissues, SM of renal vascular bed
Receptor Signaling: Stimulation of adenylate cyclase, increased cAMP Agonist Drug: Fenoldopam |
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D 2
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Location: Brain, effector tissues, SM, presynaptic nerve terminals
Receptor Signaling: Inhibition of adenylate cyclase, increased K conductance Agonist Drug: Bromocriptine |
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D 3
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Location: Brain
Receptor Signaling: Inhibition of adenylate cyclase |
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D 4
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Location: Brain, CV system
Receptor Signaling: Inhibition of adenylate cyclase |
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D 5
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Location: Brain, effector tissues, SM of renal vascular beds
Receptor Signaling: Stimulation of adenylate cyclase, increased cAMP |
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Catecholamines
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1. Phenylethylamine
2. Norepinephrine 3. Epinephrine 4. Isoproterenol 5. Dopamine |
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Alpha Agonists and Relative Affinity
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1. Phenylephrine
2. Clonidine |
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Mixed alpha & beta Agonists and Relative affinity
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1. Norepinephrine
2. Epinephrine |
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Beta Agonists and Relative Affinity
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1. Dobutamine
2. Isoproterenol 3. Albuterol, terbutaline, ritodrine |
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Endogenous Catecholamines
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1. Epinephrine
2. Norepinephrine 3. Dopamine |
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Indirect-acting Sympathomimetics
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1. Cocaine
2. Amphetamine 3. Tyramine |
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Mixed-acting Sympathomimetics
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Ephedrine
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Adrenergic Agonists
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1. Phenylephrine
2. Isoproterenol 3. Clonidine 4. Albuterol |
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Adrenergic Antagonists
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1. Prazosin
2. Propranolol 3. Metoprolol 4. Phentolamine |
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Drugs Affecting Monoamine Transporters
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1. Cocaine & methylphenidate block re-uptake by NET, stimulating alpha & beta receptors (alpha 2 receptors stimulated which inhibit NE release).
2. Amphetamine acts as substrate for NET & blocks re-uptake of NE, causes reverse transport by NET. |
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Epinephrine
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-Endogenous catecholamine
-alpha & beta agonist -potent vasoconstrictor & cardiac stimulant alpha 1 receptors in vascular beds beta 1 receptors in heart (positive ionotropic & chronotropic) beta 2 receptors in skeletal muscle (increases blood flow to muscle during exercise & decreases TPR) |
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Norepinephrine
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-endogenous catecholamine
-activates alpha 1 & 2 and beta 1 -increases BP -positive ionotropic effects on heart -positive chronotropic effects (compensatory baroreflex overcomes effect) |
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Dopamine
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-endogenous catecholamine
-activates D 1 receptors vasodilation of renal, splanchnic, coronary & cerebral arteries -used to treat oliguria (increases renal perfusion) -activates beta 1 receptors in heart -activation of presynaptic D 2 receptors suppresses NE release |
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Phenylephrine
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-direct acting
-all alpha 1 effects 1. vascular beds: vasoconstriction, increased peripheral resistance (baroreceptor reflexes decrease HR) 2. stimulation of heart: slight ionotropic effect 3. receptors in eye: mydriasis 4. nasal mucosa: vasoconstriction of vessels |
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Midodrine
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-direct acting
-prodrug: metabolized to alpha 1 agonist desglymidodrine -increases BP (treats autonominc insufficiency & postural hypotension; complication--supine HTN) |
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Clonidine
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-direct acting
-alpha 2 agonist -CNS mediated decrease in BP, slowing of HR -activates presynaptic alpha 2 receptors that suppress release of NE -abrupt D/C of long-term therapy-->withdrawal rxns -IV infusion: transient increase in BP (alpha 2 vasoconstriction) followed by hypotension partial agonist--high affinity, low efficacy |
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Guanfacine
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-direct acting
-stimulates alpha 2 receptors -causes vasodilation -greater selectivity for alpha 2 receptors than clonidine |
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Methyldopa
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-direct acting
-stimulates alpha 2 receptors -Causes vasodilation -"false transmitter" in peripheral neurons -treats HTN in pregnancy |
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Dexmedetomidine
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-direct acting
-centrally acting alpha 2 agonist -sedation of intubated or ventilated patients |
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Xylometazoline, Oxymetazoline, Propylhexedrine, and Naphazoline
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-direct acting
-alpha agonists -vasoconstriction of nasal mucosa BVs (topical decongestants) -high doses--> hypotension -"rebound effect" after long-term usage |
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Isoproterenol
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-direct acting
-potent beta receptor agonist -vasodilator (decreases BP) -positive ionotropic & chronotropic effects (increases CO) -relaxes SM (bronchial & GI) -used in asthma (mostly replaced by more selective drugs) |
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Dobutamine
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-direct acting
-beta 1 selective agonist -racemic mixture activates alpha & beta (+ and - alpha response cancel each other out) -increases CO (more so than isoproterenol) -used short-term in cardiac decompensation (CHF) |
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Albuterol, Salmeterol, Metaproterenol, Formoterol, Terbutaline
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-beta 2 selective agoinsts
-treats asthma (inhalation), relaxes bronchial SM |
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Ritodrine, Terbutaline
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-beta 2 selective agonists
-used in premature labor (relaxes uterine SM) |
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Ephedrine
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-mixed acting
-alpha & beta agonist -herbal medicines (ma huang, ephedra) contain several ephedrine-like alkaloids; banned in US -enhances release of NE from sympathetic neurons -increases HR, CO, & BP -stimulation of alpha receptors in bladder SM can increase urinary retention -activation of beta receptors in lungs promotes bronchodilation -CNS stimulant |
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Pseudoephedrine & Phenylpropanolamine
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-mixed acting
-nasal decongestants |
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Amphetamine-like
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-indirect acting
-amphetamine, methamphetamine, methylphenidate, modafinil, tyramine, phenmetrazine, phenteramine/fenfluramine |
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Amphetamine
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-indirect acting
-D isomer > L isomer CNS potency -readily enters CNS (stimulant) -stimulates mood and alertness, depresses appetite, raises BP, decreases HR (reflex slowing), increases respiration -affects dopamine transporter (DAT) and vesicular monoamine transporter 2 (VMAT2) |
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Modafinil
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-indirect acting
-treats narcolepsy -inhibits both NE & DA transporters -increases [ ] of serotonin & glutamate, decreases [ ] of GABA |
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Tyramine
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-indirect acting
-found in aged cheese, beer, & red wine -inactivated in liver by MAO normally -patient on MAOI may experience severe HTN crisis if they ingest tyramine release of stored catecholamines |
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Cocaine
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-indirect acting
-catecholamine re-uptake inhibitor -inhibits NE, DA, & serotonin re-uptake -intense psychological effects (shorter than amphetamine but more intense) -dose dependent increase in HR & BP |
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Atomoxetine and Reboxetine
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-indirect acting
-catecholamine re-uptake inhibitor -selective inhibition of NET -central effects on BP similar to clonidine -treats ADHD in children |
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Sibutramine
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-indirect acting
-catecholamine re-uptake inhibitor -inhibits NE & serotonin re-uptake -appetite suppressant approved by FDA |
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Duloxetine
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-indirect acting
-catecholamine re-uptake inhibitor -inhibits NE & serotonin re-uptake -antidepressant |
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Fenoldopam
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-D 1 receptor agonist
-vasodilation of some vascular beds -used for IV treatment of severe HTN |
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Levadopa
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-dopamine agonist
-converted to dopamine in body -used to treat Parkinson's and prolactinemia |
