Drug acting on uterus

Drugs acting on uterus

Drugs acting on uterus can primarily affect the endometrium or the
myometrium.
The most important drugs affecting endometrium are estrogens,
progestin's and their antagonists.
Myometrium receives both sympathetic and parasympathetic
innervation: autonomic drugs can affect its motility.
UTERINE STIMULANTS (Oxytocics,
Abortifacients)
These drugs increase uterine motility, especially at term.
1. Posterior pituitary hormone; Oxytocin, Desamino oxytocin
2. Ergot alkaloids; Ergometrine (Ergonovine), Methylergometrine
3. Prostaglandins; PGE2, PGF2α, 15-methyl PGF2α, Misoprostol
4. Miscellaneous Ethacridine.
 Oxytocin
Preparation: it comes in injection of 10IU ampule
Mode of action: Contracts the myoepithelial cells of the breast → milk letdown and
ejection,
- Contracts the uterus → delivery; The uterus is insensitive to oxytocin in early pregnancy
but its sensitivity increases with advanced pregnancy reaching maximum at time of delivery.
Pharmacokinetics
Oxytocin is inactive orally
Administered by i.m. or i.v. routes, rarely by intranasal spray.
Rapidly degraded in liver and kidney
Plasma t½ 6–12 min,
Pregnant uterus and placenta elaborate a specific aminopeptidase called oxytocinase
Unitage and preparations: 1 IU of oxytocin = 2 μg of pure hormone.
 Dosage:
• Induction and augmentation of labour: Dilute 5 IU in 500 ml or 10 IU in 1 litre
of Ringer lactate or 0.9% sodium chloride to obtain a solution of 10 milliunits
per ml. Start an infusion of 5 drops/minute, then increase by 5 drops/minute
every 30 minutes (max. 60 drops/minute) until efficient contractions are
obtained (3 to 4 contractions lasting 40 seconds over 10 minutes).
• Treatment of postpartum haemorrhage due to uterine atony: 20 IU in 1 litre of
Ringer lactate or 0.9% sodium chloride, administered over 2 hours (160
drops/minute). Simultaneously, 5 to 10 IU by slow IV injection, to be repeated if
necessary until the uterus is retracted (max. total dose 60 IU).
• Prevention of postpartum haemorrhage (vaginal delivery): 5 to 10 IU by slow
IV or IM injection before or after the delivery of placenta.
• Prevention of postpartum haemorrhage (caesarean section): 10 IU by slow IV
injection after cord clamping, then 20 UI in 1 litre of Ringer lactate or 0.9%
sodium chloride, administered over 2 hours (160 drops/minute).
Clinical uses to oxytocin: • Induction of labor Drug of choice • Postpartum
hemorrhage (I.M. Ergot alkaloids are better) • Breast engorgement (intranasally)
 contraindication: Do not administer by rapid IV injection (risk of hypotension with
flushing and reflex tachycardia, uterine hypertonia and/or rupture, foetal distress).
- During labour:
Do not administer to patients with history of two caesarean sections or more.
- Administer with caution and do not exceed 30 drops/minute in patients with
history of single caesarean section and in grand multipara (risk of uterine rupture).
Respect the dosage and rate of administration, monitor uterine contractility and
foetal heart rate.
Side effects to oxytocin: • Rupture of the uterus is a Major and most serious side
effect • H2O intoxication and hypertension Due to its ADH-like activity • Specific
oxytocin antagonist Atosiban, effective in the management of premature delivery
Ergometrine
Preparation: it comes in 0.5mg ampoules and 500mcg(0.5mg) tablets
Action: it causes uterine contraction leading to prevention or
controlling PPH
Indication: prevention and control of PPH, control of PV bleeding
after Abortion and D&C
Dose: 0.5mg IM, IV, PO after 2nd stage labour
Contraindication: should never be given before the end of 2nd stage
lobour, severe cardiac disease, severe hepatic disease, severe renal
impairment, severe hypertension, eclampsia.
 Side effects
• Nausea and vomiting, headache, dizziness, tinnitus (buzzing in the
ears), abdominal pain, dyspnoea, bradycardia.

• Syntometrine: this is a combination of Oxytocin and ergometrine

• It contains 0.5mg ergometrine and 5iu of oxytocin in 1ml ampoule.
Dosage: 1ml IM or IV after 2nd stage of labour.
Indication: prevention and control of PPH
Contraindication: as for above drugs.
Side effects: as for individual drugs.
Misoprostol
Pharmacological class; prostaglandins E1 analog
Preparation: 25mcg and 200mcg tablets
Pharmacokinetics: is rapidly absorbed after oral administration and
undergoes rapid de-esterification to its active form misoprostol acids.
And further Metabolized by oxidation in the liver and excreted in the
urine about 80% and some in breast milk.
Route of administration: Oral (onset 8min), sublingual (11min),
vaginal (3 hours), Rectal (4hours)
 Dosage and Duration:
• Incomplete abortion: Up to 13 weeks since the last menstrual period: 400
micrograms single dose sublingually or 600 micrograms single dose orally
• From 13 to 22 weeks since the last menstrual period: 400 micrograms sublingually
every 3 hours
• Termination of pregnancy: Up to 13 weeks since the last menstrual period: 800
micrograms single dose sublingually or vaginally. If expulsion has not occurred within
24 hours administer a 2nd dose of 800 micrograms.
• From 13 to 22 weeks since the last menstrual period: 400 micrograms single dose
sublingually or vaginally every 3 hours
• Induction of labour: 25 micrograms orally every 2 hours, or if not possible, vaginally
every 6 hours, until labour starts (max. 200 micrograms per 24 hours)
• Treatment of post-partum haemorrhage: 800 micrograms single dose sublingually
• Cervical dilation before aspiration or curettage: 400 micrograms single dose
sublingually 1 to 3 hours before the procedure or vaginally 3 hours before the
procedure
  Indication
• missed or incomplete abortion
• Induction in the first & second trimester
• Labor induction with both alive &dead fetus.
• Prevention &Treatment of postpartum hemorrhage
•Cervical ripening before; (Surgical abortion in the first or second trimester,
Hysteroscopy, Dilation of cervix)
Contraindication and precaution: For induction of labour if the foetus is viable: Do
not administer in the event of previous caesarean section. Administer with caution in
case of grand multiparity or overdistention of the uterus (risk of uterine rupture). Do
not administer simultaneously with oxytocin. At least 4 hours apart. No
contraindication in breastfeeding
Side effects: Chills; constipation; diarrhoea; dizziness; fever; flatulence;
gastrointestinal discomfort; headache; nausea; skin reactions; less urination, foetal
heart rhythm disorders, foetal distress. It is dose dependent effects.