Drug Study

Functional Class: Chemical Class: Generic Name:

Sympathomimetic Amine Adrenergic Agonist Ephedrine

Mechanism of Action: Ephedrine is a sympathomimetic amine. The principal mechanism of its action relies on its indirect stimulation of theadrenergic receptor system, which is part of the sympathetic nervous system (SNS), by increasing the activity of noradrenaline at the post-synaptic - and -receptors. The presence of direct interactions with -receptors is unlikely, but still controversial. L-Ephedrine, and particularly its stereoisomer norpseudoephedrine(which is also present in Catha edulis) has indirect sympathomimetic effects and due to its ability to cross the blood brain barrier, it is a CNS stimulant similar toamphetamines but less pronounced, as it releases noradrenaline and dopamine in the substantia nigra. The presence of an N-methyl group decreases binding affinities at -receptors, compared with norephedrine. On the other hand ephedrine binds better than Nmethylephedrine, which has an additional methyl group at the N-atom. Also the steric orientation of the hydroxyl group is important for receptor binding and functional activity. Contraindications: Angle-closure glaucoma; patients anesthetized with cyclopropane or halothane; cases in which vasopressor drugs are contraindicated (eg, thyrotoxicosis, diabetes mellitus, hypertension of pregnancy); MAOI therapy; narrow-angle glaucoma; nonanaphylactic shock during general anesthesia with halogenated hydrocarbons or cyclopropane. Children: Oral, S.C.: 3 mg/kg/day or 25-100 mg/m2/day in 4-6 divided doses every 4-6 hours I.M., slow I.V. push: 0.2-0.3 mg/kg/dose every 4-6 hours Adults: Oral: 25-50 mg every 3-4 hours as needed I.M., S.C.: 25-50 mg, parenteral adult dose should not exceed 150 mg in 24 hours I.V.: 5-25 mg/dose slow I.V. push repeated after 5-10 minutes as needed, then every 3-4 hours not to exceed 150 mg/24 hours Dosage Form: Capsule, as sulfate: 25 mg, 50 mg Injection, as sulfate: 25 mg/mL (1 mL); 50 mg/mL (1 mL, 10 mL) Jelly, as sulfate (Kondon's Nasal): 1% (20 g) Spray, as sulfate (Pretz-D): 0.25% (15 mL) Decreased effect: Alpha- and beta-adrenergic blocking agents decrease ephedrine vasopressor effects Increased toxicity: Additive cardiostimulation with other sympathomimetic agents; theophylline cardiostimulation; MAO inhibitors or atropine may increase blood pressure; cardiac glycosides or general anesthetics may increase cardiac stimulation. Nervousness, anxiety, apprehension, fear, tension, agitation, excitation, restlessness, irritability, insomnia, hyperactivity, chest pain, arrhythmias & dyspnea

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Cardiovascular: Hypertension, tachycardia, palpitations, elevation or depression of blood pressure, unusual pallor Central nervous system: Dizziness, headache Gastrointestinal: Xerostomia, nausea, anorexia, GI upset, vomiting Genitourinary: Painful urination Neuromuscular & skeletal: Trembling, tremor (more common in the elderly), weakness Miscellaneous: Diaphoresis (increased) Assess I&O Assess EKG continuously during administration Assess B/P and heart rate every 5 minutes Assess for paresthesias and coldness of extremities. Peripheral blood flow may decrease. Long term use may produce anxiety states requiring sedation. Increased lactic acid with sever metabolic acidosis can occur. Assess the injection site for tissue sloughing and administer phentolamine mixed in NS if this occurs. If given IV, give through a stopcock or Y-connection, inject 10-25mg slowly. May be given undiluted. Protect solution from light. Monitor potassium levels May cause anoxia in the fetus Safety for use in breast-feeding is not established.

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Drug Study Functional Class: Chemical Class: Generic Name: Beta-sympathomimetic Beta-Adrenergic Agonist Isoproterenol

Mechanism of Action: The pharmacologic effects of isoproterenol are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic AMP. Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. Contraindications: Use of isoproterenol hydrochloride injection is contraindicated in patients with tachyarrhythmias; tachycardia or heart block caused by digitalis intoxication; ventricular arrhythmias which require inotropic therapy; and angina pectoris. Children: Bronchodilation: Inhalation: Metered dose inhaler: 1-2 metered doses up to 5 times/day Bronchodilation (using 1:200 inhalation solution) 0.01 mL/kg/dose every 4 hours as needed (maximum: 0.05 mL/dose) diluted with NS to 2 mL Sublingual: 5-10 mg every 3-4 hours, not to exceed 30 mg/day Cardiac arrhythmias: I.V.: Start 0.1 mcg/kg/minute (usual effective dose 0.2-2 mcg/kg/minute) Adults: Bronchodilation: Inhalation: Metered dose inhaler: 1-2 metered doses 4-6 times/day Bronchodilation: 1-2 inhalations of a 0.25% solution, no more than 2 inhalations at any one time (1-5 minutes between inhalations); no more than 6 inhalations in

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any hour during a 24-hour period; maintenance therapy: 1-2 inhalations 4-6 times/day. Alternatively: 0.5% solution via hand bulb nebulizer is 5-15 deep inhalations repeated once in 5-10 minutes if necessary; treatments may be repeated up to 5 times/day. Sublingual: 10-20 mg every 3-4 hours; not to exceed 60 mg/day Cardiac arrhythmias: I.V.: 5 mcg/minute initially, titrate to patient response (2-20 mcg/minute) Shock: I.V.: 0.5-5 mcg/minute; adjust according to response Dosage Form: Inhalation: Aerosol: 0.2% (1:500) (15 mL, 22.5 mL); 0.25% (1:400) (15 mL) Solution for nebulization: 0.031% (4 mL); 0.062% (4 mL); 0.25% (0.5 mL, 30 mL); 0.5% (0.5 mL, 10 mL, 60 mL); 1% (10 mL) Injection: 0.2 mg/mL (1:5000) (1 mL, 5 mL, 10 mL) Tablet, sublingual: 10 mg, 15 mg headache, dizziness, lightheadedness, or insomnia;tremor or nervousness,sweating; nausea, vomiting, or diarrhea; or dry mouth. Insomnia, restlessness dry throat, xerostomia, discoloration of saliva (pinkish-red) Assess History: Hypersensitivity to isoproterenol; tachyarrhythmias; general a nesthesia with halogenated hydrocarbons or cyclopropane; unstable vasomotor system disorders; hypertension; coronary artery disease; history of stroke; COPD patients with degenerative heart disease; diabetes mellitus; hyperthyroidism; history of seizure disorders; psychoneurotic individuals; labor and delivery; lactatation Physical: Weight; skin color, temperature, turgor; orientation, reflexes; P, BP; R, adventitious sounds; blood and urine glucose, serum electrolytes, thyroid function tests, ECG Use minimal doses for minimum periods; drug tolerance can occur with prolonged use. Maintain a -adrenergic blocker (a cardioselective -blocker, such as atenolol, should be used in patients with respiratory distress) on standby in case cardiac arrhythmias occur. Do not exceed recommended dosage of inhalation products; administer pressurized inhalation drug forms during second half of inspiration, because the airways are open wider and the aerosol distribution is more extensive. If a second inhalation is needed, give at peak effect of previous dose, 3---5 min.

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Holy Trinity University College of Nursing and Health Sciences Puerto Princesa City

In Partial Fulfillment of the Requirements In PHARMACOLOGY

Submitted to: MRS. RACHEL M. ITOK, RN, MAN Of Holy Trinity University

Presented by: De Leon, Diana Laura Lei, V. Sabroso, Donisa, G.