SYMPHATOMIMETICS AS TOCOLYTIC AGENT

Siti Syarifah Prog. Study of Biomedic Faculty of Medicine, University Sumatera Utara Medan, 2012

INTRODUCTION

Tocolysis : The inhibition of myometrial contractions Tocolytic agent : drug administered to inhibit myometrial contraction The agent approved by FDA was Ritodrine (1980) One of -Adrenergic receptor agonists

-Adrenergic receptor

-3 receptors: promote lypolisis

STRUCTURE AND GENERAL CHARACTERISTIC

G-protein couple receptors The rank order in term of potency: isoproterenol > epinephrine > norepinephrine

RITODRINE

((R,S)-4-hydroxy-alpha-[1-[2-((4hydroxyphenyl)ethyl}amino)ethyl]benzenemethanol Molecular Formula: C17H21NO3 Trade/Brand name: Yutopar ROA: PO tablet 10 mg, parenteral 10 mg/ml

PHARMACOKINETIC

Absorption Rapid absorption from the GI tract (oral). Bioavailability: about 30% of an oral dose. Distribution Crosses the placenta. Metabolism Hepatic: By conjugation with glucuronic acid or sulfate. Excretion 70-90% of a dose is excreted in the urine within 10-12 hours.

PHARMACODYNAMIC

Indication: Preterm Labour/ Preterm birth defined as birth before the completion of 37 weeks of gestation the process itself is generally heralded by synchronous changes in the myometrium and cervix that permit expulsion of the fetus

MECHANISM OF ACTION

DOSE
I V infusion: Initial dose 0,05 mg/min to be gradually increased according to the results by 0,05 mg/min every 10-15 min until the desired results is attained, max 0,3 mg/min. Oral: - Maintenance: 1 tab 2 hrly during the 1st day, max 12 tab - Thereafter 1-2 tab 4-6 hrly. Max: 80-120 mg daily

ADVERSE EFFECT

Tachycardia and hypotension Tremor Palpitasi Shortness of breath Chest discomfort Pulmonary edema Hypokalemia Hyperglicemia

DRUG INTERACTION

--G.Anesth., Pethidine,or MgSO4 : Arrhythmia& hypotension

-Atropine : Increase B.P. -B Blockers : Decrease tocolytic effect. -Asthmatic patients under B.Adrenergics: Tachyphlaxis(drug resistance)

-Diabetic patients : MgSO4 : Pulmonary edema Corticosteroids orInsulin Antagonist ( insulin

CONTRAINDICATIONS

Absolute: Maternal cardiac disease, eclampsia, severe pre-eclampsia, hemorrhage, uncontrolled hyperthyroid, diabetes Relative: Diabetes, hypertension, migraines, sepsis