SYNTOMETRINE INJECTION

Product Information

Registration Status: Active

SYNTOMETRINE INJECTION is approved to be sold in Singapore with effective from 1989-05-07. It is marketed by PHARMACON PTE LTD, with the registration number of SIN03588P.

This product contains Ergometrine 0.5mg/ml, and Oxytocin 5 iu/ml in the form of INJECTION. It is approved for INTRAVENOUS, INTRAMUSCULAR use.

This product is manufactured by ROTEXMEDICA GMBH in GERMANY.

It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Ergometrine
Oxytocin

Description

An ergot alkaloid with uterine and vascular smooth muscle contractile properties.

Indication

Used to treat postpartum haemorrhage and postabortion haemorrhage in patients with uterine atony.

Mechanism of Action

Ergonovine directly stimulates the uterine muscle to increase force and frequency of contractions. With usual doses, these contractions precede periods of relaxation; with larger doses, basal uterine tone is elevated and these relaxation periods will be decreased. Contraction of the uterine wall around bleeding vessels at the placental site produces hemostasis. Ergonovine also induces cervical contractions. The sensitivity of the uterus to the oxytocic effect is much greater toward the end of pregnancy. The oxytocic actions of ergonovine are greater than its vascular effects. Ergonovine, like other ergot alkaloids, produces arterial vasoconstriction by stimulation of alpha-adrenergic and serotonin receptors and inhibition of endothelial-derived relaxation factor release. It is a less potent vasoconstrictor than ergotamine. As a diagnostic aid (coronary vasospasm), ergonovine causes vasoconstriction of coronary arteries.

Pharmacokinetics

Absorption
Absorption is rapid and complete after oral or intramuscular administration.
Distribution
Metabolism
Hepatic.
Elimination

Toxicity

The principal symptoms of overdose are convulsions and gangrene. Other symptoms include bradycardia, confusion, diarrhoea, dizziness, dyspnoea, drowsiness, fast and/or weak pulse, miosis, hypercoagulability, loss of consciousness, nausea and vomiting, numbness and coldness of the extremities, pain in the chest, peripheral vasoconstriction, respiratory depression, rise or fall in blood pressure, severe cramping of the uterus, tachycardia, tingling, and unusual thirst.

Active Ingredient/Synonyms

(6aR,9R)-7-Methyl-4,6,6a,7,8,9-hexahydro-indolo[4,3-fg]quinoline-9-carboxylic acid ((S)-2-hydroxy-1-methyl-ethyl)-amide | [8β(S)]-9,10-didehydro-N-(2-hydroxy-1-methylethyl)-6-methylergoline-8-carboxamide | 9,10-didehydro-N-(2-hydroxy-1-methylethyl)-6-methylergoline-8β(S)-carboxamide | 9,10-didehydro-N-(α-(hydroxymethyl)ethyl)-6-methylergoline-8-β-carboxamide | D-lysergic acid 1-hydroxymethylethylamide | D-lysergic acid-L-propanolamide | Ergobasine | Ergometrina | Ergometrine | Ergométrine | Ergometrinum | Ergonovine | Ergotocine | Margonovine | N-(2-Hydroxy-1-methylethyl)-D-(+)-lysergamide | N-(α-(hydroxymethyl)ethyl)-D-lysergamide | Ergonovine |


Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.


Description

Synthetic 9 residue cyclic peptide. The hormone is prepared synthetically to avoid possible contamination with vasopressin (ADH) and other small polypeptides with biologic activity.

Indication

Used for labor induction, augmentation of labor, postpartum abbreviation of third stage of labor, postpartum control of uterine bleeding, termination of pregnancy and for the evaluation of fetal respiratory capability. Oxytocin cannot be used for elective induction of labor, there must be a clear medical requirement.

Mechanism of Action

Uterine motility depends on the formation of the contractile protein actomyosin under the influence of the Ca2+-dependent phosphorylating enzyme myosin light-chain kinase. Oxytocin promotes contractions by increasing the intracellular Ca2+, which in turn activates myosin's light chain kinase.. Oxytocin has specific receptors in the muscle lining of the uterus and the receptor concentration increases greatly during pregnancy, reaching a maximum in early labor at term.

Pharmacokinetics

Absorption
Uterine response after IV administration is immediate and subsides after 1 hour. Uterine contractions occur 3-5mins after IM administration and decreases within 2-3 hours. When 100-200milliunits is administered IV, contractions of the myoepithelial tissue surrounding the alveoli of the breasts occur within minutes and last for about 20 mins.
Distribution
Distributes throughout the extracellular fluid and crosses the placenta. It is probable that it also distributes into milk in small amounts.
Metabolism
Oxytocin is rapidly metabolized in the liver and also in the plasma by oxytocinases. It is also metabolized to a smaller degree by the mammary glands.
Elimination

Toxicity

Oxytocin can produce a severe water intoxication due to its antidiuretic effect. Prolonged IV infusions of more 40milliunits/min are usually the cause. Severe water intoxication with convulsions, coma, and death can occur. Some neonatal seizures have also been reported. Consider potential for water intoxication, particularly when administered by IV infusion and patient is receiving oral fluids. Uterine effects: High doses or hypersensitivity to oxytocin may cause uterine hypertonicity, spasm, tetanic contraction, or rupture of the uterus. There have also been reported allergic and anaphylactic reactions to oxytocin but they were rarely fatal.

Active Ingredient/Synonyms

Oxytocin | Oxytocin |


Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank