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Adrenergic Drugs Flashcards

(50 cards)

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1
Q

Direct-acting Selective Adrenergic Agonists

A
  • a1-phenylephrine
  • a2-clonidine
  • B1-dobutamine
  • B2-terbutaline

Responses are not reduced by prior treatment w/ reserpine or guanethidine. Response may be potentiated by cocaine, reserpine and guanethidine.

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2
Q

Direct-acting Non-selective Adrenergic Agonists

A
  • a1 a2-oxymetazoline
  • B1 B2-isoproterenol
  • a1 a2 B1 B2-epinephrine
  • a1 a2 B1-norepinephrine

Responses are not reduced by prior treatment w/ reserpine or guanethidine. Response may be potentiated by cocaine, reserpine and guanethidine.

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3
Q

Mixed-acting Adrenergic Agonists

A
  • ephedrine (a1 a2 B1 B2 and releasing agent)

Response is reduced by prior treatment w/ reserpine or guanethidine.

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4
Q

Indirect-acting Adrenergic Agonist Releasing Agents

A
  • amphetamine
  • tyramine

Responses are abolished by prior treatment w/ reserpine or guanethidine

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5
Q

Indirect-acting Adrenergic Agonists Uptake Inhibitor

A
  • cocaine
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6
Q

Indirect-acting Adrenergic Agonist MOA Inhibitors

A
  • selegiline
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7
Q

Indirect-acting Adrenergic Agonist COMT Inhibitors

A
  • entacapone
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8
Q

Alpha1 Receptors Actions

A
  • alpha 1 postsynaptic receptors mediate smooth muscle contraction
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9
Q

Alpha2 Receptors Actions

A
  • presynaptic receptors negative feedback inhibition of neuronal NE release
  • extrajunctional receptors (noninnervated) which respond to circulating catecholamines, mediate smooth muscle contraction
  • central postsynaptic receptors in braine stem mediate reduction in sympathetic outflow
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10
Q

Order of Adrenergic Agonist Potentcy

A

Although the naturally occuring catecholamines cannot distinguish b/w a1 and a2 subtypes, many synthetic drugs do

  • EPI>NE>DA (dopamine)>ISOP (isoproterenol)
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11
Q

Beta1 Receptors Actions

A
  • B1 postsynaptic receptors mediate cardiac stimulation and renin release
  • ISOP>EPI=NE>DA
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12
Q

Beta2 Receptors Actions

A
  • B2 postsynaptic receptors mediate smooth muscle relaxation
  • ISOP>EPI>NE
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13
Q

NE Receptors w/ Major Pharmacological Effects

A
  • a1 and 2 (a1 is clinically significant), B1 (variable)
  • NE inactivated after PO adm; duration of action is extremely short due to MAO and COMT metabolism
  • Clinical indications: used in shock (IV) to inc. BP, slow drip
  • Adverse effects: inc. BP/hypertensive crisis/hemorrhage, reflex bradycardia, excessive nasal dryness, blurred vision, IV infiltration > tissue necrosis (may be treated w/ alpha antagonist phentolamine)
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14
Q

EPI Receptors w/ Major Pharmacological Effects

A
  • a1 and 2
  • B1 and 2
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15
Q

ISOP Receptors w/ Major Pharmacological Effects

A
  • B1 and 2
  • very little alpha (clinically nonsignificant)
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16
Q

Structure activity relationships of sympathomimetic amines

A
  • C-3, C-4 (catecholamines): COMT metabolizes (short drug action)
  • C-3, C-5 (B2 selectivity): COMT does not metabolize (long duration of action)
  • lack of OH group: increases lipid solubility for CNS penetration and COMT does not metabolize (long duration of action)
  • Nitrogen substitution: increases beta selectivity
  • Alpha-carbon substitution: MAO does not metabolize (long drug action)
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17
Q

Alpha-1 agonist intracellular actions

A
  • Stimulates Gq and increases IP3 and DAG, further enhances intracellular calcium, causes vasoconstriction (pressor effects)
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18
Q

Phenylephrine

A
  • PO, nasal, IV; pressor decongestant, mydriatic
  • Stimulates alpha1 receptors, little or no beta effect; primarily vasoconstrictor
  • Not a catecholamine, duration of action: 30-60min

Clinical Indications

  • IV to inc BP
  • PO or intranasally as decongestant
  • Opthalmic drops for mydriasis

Adverse Effects

  • Cardiovascular system (CVS)- increase in blood pressure, cardiac failure and arrhythmia
  • Infiltration necrosis after parenteral administration
  • Rebound nasal congestation
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19
Q

Naphazoline and Oxymetazoline

A
  • Naphazoline: a1 agonist
  • Oxymetazoline: non-selective alpha agonist
  • PO or intranasally as nasal decongestant
  • Relief of redness of eye (naphazoline, oxymetazoline)
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20
Q

Clonidine

A
  • Alpha2 agonist
  • Stimulates presynaptic a2 receptors in CNS to decrease sympathetic outflow to the periphery

Clinical Uses

  • Hypertenstion
  • Withdrawal symptoms from opiates, tobacco smoking, and benzodiazepines

Side Effects

  • Lethargy, sedation, constipation and dry mouth
  • Abrupt discontinuance causes reboud hypertension
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21
Q

Ephedrine and pseudoephedrine

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A
  • Mixed acting agonists; PO, decongestant
  • Ephedrine-containing herbal supplements banned du to life-threatening cardiovascular reactions
  • Phenylephrine has replaced pseudophedrine in many oral decongestants, since pseudoephedrine has been misused to make meth
22
Q

Other indirect or mixed action adrenergic agonists

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A
  • Phentermine: PO; anoretic
  • Phenylpropanolamine: PO, decongestant, anorectic
23
Q

Beta1 receptor intracellular actions

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A
  • Stimulation activates Gs protein to increase intracellular cAMP, which further increases intracellular Ca to increase contractility in heart and renin release in kidney
24
Q

Beta2 receptor intracellular actions

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A
  • Present in smooth muscle; stimulation results in activation of Gs protein to increase intracellular cAMP and phosphorylation of myosin light chain kinase (MLCK) and cause muscle relaxation
25
Isoproterenol
**_Drug Effects_** - Non-selective, stimulates beta1 and 2, parenteral, inhalation, sublingual - Causes vasodilation within the skeletal muscles, resulting in a drop in total peripheral resistance and a concurrent drop in diastolic pressure - Chronotropic actions resulting in a rise in systolic pressure - Glycogenolysis and hyperlipidemia and myometrial relaxation **_Clinical Indications_** - Mainly used to treat heart block, bradycardia, ventricular arrhythmia (torsades de pointes); In disorder such as asthma and shock, isoproterenol largely has been replaced by other sympathomimetic drugs **_Adverse Effects_** - Tachycardia, palpitations, arrhytmias, inc BP, tremors - CNS stimulation/anxiety in overdoses
26
Dobutamine
- Selective beta1 agonist at therapeutic doses - Incs force \> heart rate at therapeutic conc.; different isomers have opposing effects on alpha 1 receptors - Used parenterally in acute CHF - Development of tolerance w/ prolonged use - Adverse effects: develop ventricular arrhythmia
27
Terbutaline
- Selective beta2 agonist - PO, SC, inhalation or parenteral (IV), lasts 3-6hrs - Relaxes smooth muscle, bronchodilation, relax uterus in premature labor, vasodilation skeletal muscle blood vessels **_Clinical Indications_** - Use for asthma, acute bronchospasm; inhibit the uterine contractions assoc. w/ premature labor **_Adverse Effects_** - Tremor, tachycardia (at higher doses can cause some beta-1 stimulation on heart)
28
Albuterol
- Selective beta2 agonist - PO, inhalation, short-acting
29
Epinephrine (ADRENALINE)
- Parenteral; inhalation, IM, SC - alpha and beta receptor stimulator - **alpha1** stimulation: causes a rise in systolic blood pressure due to regional vasoconstriction - **alpha2** stimulation: causes decreased release of insulin - **beta1** stimulation: causes a rise in systolic pressure due to an increased cardiac output (heart rate and contractility increase) - **beta2** stimulation: causes a drop in diastolic pressure due to skeletal muscle vasodilation, bronchorelaxation, hyperglycemic effect (increased glycogenolysis in liver), and increased release of glucagon - Lipolysis: hydrolyzes triglycerides to free fatty acids and glycerol **_Clinical Indications_** - Blood pressure, heart (cardiac stimulant), smooth muscle (asthma), mast cells (antiallergic effect, especially for anaphylaxis), topical hemostatic agent (eg. bleeding peptic ulcers), calorigenic effect (metabolic); hyperglycemis, inc. free fatty acids, insulin- alpha vs. beta effect **_Adverse Effects_** - CVS- ventricular arrhytmias - CNS- headache, restlessness
30
Dopamine (INTROPIN)
- IV infusion Peripheral dopamine receptors (dopaminergic) - Renal- vasodilation - Mesenteric- vasodilation Dose-response relationship of dopamine and receptors - Low-dose- dopaminergic (vasodilation) - Medium dose- beta1 (force\>rate) - High dose- alpha (vasoconstriction) Uses - Circulatory shock - Acute heart failure Adverse effects - Tachycardia, anginal pain, arrhythmias, headache
31
Fenoldopam
- An intravenous dopamine D1 agonist used for the acute treatment of severe hypertension
32
Tyramine
- Indirect sympathomimetic - Releases norepinephrine from storage granules, thus producing both alpha and beta stimulation - Leads to tachyphylaxis, because of depletion of norepinephrine stores after repeated use - Hypertensive crisis (cheese effect) in patients who are taking MAO inhibitors when tyramine is ingested (fermented foods, wine) - Often used experimentally to understand mechanisms
33
Amphetamine
- Indirect sympathomimetic - Releases norepinephrine, epinephrine and dopamine (brain) Uses - CNS stimulant: stimulates mood and alertness - Appetite suppression - ADHD disorder in children: methylphenidate is preferable Adverse Effects (due to sympathomimetic effects) - Nervousness, insomnia, anorexia - Growth inhibition (children)
34
Adrenergic non-selective alpha receptor antagonists
- Phenoxybenzamine - Phentolamine
35
Adrenergic alpha1-selective antagonists
- Prazosin
36
Adrenergic non-selective beta receptor antagonists
- Nadolol - Pindolol - Propanolol - Timolol
37
Adrenergic beta1-selective antagonists
- Acebutolol - Esmolol - Metoprolol
38
Adrenergic non-selective beta receptor antagonist
- Carvedilol - Labetalol
39
Drugs which block both alpha-1 and 2 receptors
- Phenoxybenzamine - Phentolamine Main pharmacologic effects - blood vessels - heart
40
Drugs which block only alpha-1 receptors
- Prazosin
41
Alpha blockers therapeutic uses
- Diagnosis and treatment of pheochromocytoma - Shock - Peripheral vascular disease (Raynaud's) - Hypertension - Vasodilator therapy in CHF - Urinary obstruction
42
Alpha blockers adverse effects
- Nasal stuffiness - Miosis - Postural hypotension - Reflex tachycardia - Inhibition of ejaculation - Diarrhea - Epinephrine reversal
43
Beta blockers chart
44
Factors related to the use of beta blockers
- Selectivity- beta blockers can precipitate severe bronchospasm in patients w/ obstructive pulmonary disease and can mask symptoms of hypoglycemia in insulin-dependent diabetics - In low doses effects are mostly limited to the heart. In doses used to treat hypertension, can cause bronchospasm, but are still less likely to mask the symptoms of hypoglycemia - Lipid solubility - Membrane- stabilizing activity - Intrinsic sympathomimetic activity (partial agonists) beta-blockers w/ partial agonist (intrinsic sympathomimetic) activity not only block the access of catecholamines to beta-receptors but also partially activate the receptors. They cause less slowing of the heart rate at rest than other beta-blockers and may be less likely to cause serum lipid abnormalities
45
Beta blockers pharmacologic effects
- Heart - Blood pressure - CNS - Metabolic - Uterus - Renin
46
Beta blockers Therapeutic uses
- Hypertension - Cardiac arrhythmias - Angina pectoris - Glaucoma - Migraine - Pheochromocytoma - Decrease mortality after MI
47
Beta blockers adverse effects/potential problems
- GI hyperactivity - Cardiovascular: CHF, angina, arrhythmia, hypotension; should avoid abrupt drug withdrawal - Respiratory distress/asthma - CNS: insomnia, nightmares, depression - Aggravation of peripheral vascular disease - Hypoglycemia, especially following insulin administration
48
Labetalol and carvedilol
- Selective alpha-1 blocker and nonselective beta blocker Uses - Labetalol: IV for hypertension and hypertensive emergencies, pheocromocytoma - Carvedilol: used for heart failure Adverse Effects - Combination of alpha/beta blockade, hepatic injury
49
Reserpine
- Adrenergic neuronal blocker - MOA: blocks vesicular amine transporters Pharmacologic effects - Cardciovascular - CNS Therapeutic uses - Systemic hypertension Adverse effects - Orthrostatic hypotension, sedation, depression
50
Guanethidine and Gunadrel
- MOA: displaces NE from storage vesicles; acts as false transmitter Therapeutic Uses - Systemic hypertension Adverse Effects - Orthrostatic hypotension, sedation
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