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CRP > Adrenergic Drugs > Flashcards

Adrenergic Drugs Flashcards

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

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

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

Beta1 receptor intracellular actions

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

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
Q

Isoproterenol

A

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
Q

Dobutamine

A
  • 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
Q

Terbutaline

A
  • 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
Q

Albuterol

A
  • Selective beta2 agonist
  • PO, inhalation, short-acting
29
Q

Epinephrine (ADRENALINE)

A
  • 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
Q

Dopamine (INTROPIN)

A
  • 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
Q

Fenoldopam

A
  • An intravenous dopamine D1 agonist used for the acute treatment of severe hypertension
32
Q

Tyramine

A
  • 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
Q

Amphetamine

A
  • 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
Q

Adrenergic non-selective alpha receptor antagonists

A
  • Phenoxybenzamine
  • Phentolamine
35
Q

Adrenergic alpha1-selective antagonists

A
  • Prazosin
36
Q

Adrenergic non-selective beta receptor antagonists

A
  • Nadolol
  • Pindolol
  • Propanolol
  • Timolol
37
Q

Adrenergic beta1-selective antagonists

A
  • Acebutolol
  • Esmolol
  • Metoprolol
38
Q

Adrenergic non-selective beta receptor antagonist

A
  • Carvedilol
  • Labetalol
39
Q

Drugs which block both alpha-1 and 2 receptors

A
  • Phenoxybenzamine
  • Phentolamine

Main pharmacologic effects

  • blood vessels
  • heart
40
Q

Drugs which block only alpha-1 receptors

A
  • Prazosin
41
Q

Alpha blockers therapeutic uses

A
  • Diagnosis and treatment of pheochromocytoma
  • Shock
  • Peripheral vascular disease (Raynaud’s)
  • Hypertension
  • Vasodilator therapy in CHF
  • Urinary obstruction
42
Q

Alpha blockers adverse effects

A
  • Nasal stuffiness
  • Miosis
  • Postural hypotension
  • Reflex tachycardia
  • Inhibition of ejaculation
  • Diarrhea
  • Epinephrine reversal
43
Q

Beta blockers chart

A
44
Q

Factors related to the use of beta blockers

A
  • 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
Q

Beta blockers pharmacologic effects

A
  • Heart
  • Blood pressure
  • CNS
  • Metabolic
  • Uterus
  • Renin
46
Q

Beta blockers Therapeutic uses

A
  • Hypertension
  • Cardiac arrhythmias
  • Angina pectoris
  • Glaucoma
  • Migraine
  • Pheochromocytoma
  • Decrease mortality after MI
47
Q

Beta blockers adverse effects/potential problems

A
  • 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
Q

Labetalol and carvedilol

A
  • 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
Q

Reserpine

A
  • Adrenergic neuronal blocker
  • MOA: blocks vesicular amine transporters

Pharmacologic effects

  • Cardciovascular
  • CNS

Therapeutic uses

  • Systemic hypertension

Adverse effects

  • Orthrostatic hypotension, sedation, depression
50
Q

Guanethidine and Gunadrel

A
  • MOA: displaces NE from storage vesicles; acts as false transmitter

Therapeutic Uses

  • Systemic hypertension

Adverse Effects

  • Orthrostatic hypotension, sedation

CRP (16 decks)

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