The document discusses drugs that affect uterine muscle contractility. It describes oxytocin, ergot alkaloids, and prostaglandins as drugs that produce uterine contractions and their mechanisms, uses, and differences. It also discusses beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors as drugs that produce uterine relaxation and their mechanisms and side effects.
The document discusses drugs that affect uterine muscle contractility. It describes oxytocin, ergot alkaloids, and prostaglandins as drugs that produce uterine contractions and their mechanisms, uses, and differences. It also discusses beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors as drugs that produce uterine relaxation and their mechanisms and side effects.
The document discusses drugs that affect uterine muscle contractility. It describes oxytocin, ergot alkaloids, and prostaglandins as drugs that produce uterine contractions and their mechanisms, uses, and differences. It also discusses beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors as drugs that produce uterine relaxation and their mechanisms and side effects.
The document discusses drugs that affect uterine muscle contractility. It describes oxytocin, ergot alkaloids, and prostaglandins as drugs that produce uterine contractions and their mechanisms, uses, and differences. It also discusses beta-adrenoceptor agonists, calcium channel blockers, and prostaglandin synthetase inhibitors as drugs that produce uterine relaxation and their mechanisms and side effects.
3. PROSTAGLANDINS a) PGE2 b) PGF2α OXYTOCIN R (Syntocinon )
Synthesis
• Is a posterior pituitary hormone secreted by the
posterior pituitary gland.
• Oxytocin secretion occurs by sensory stimulation
from cervix ,vagina , and from suckling at breast. Pharmacokinetics of oxytocin Absorption ,Metabolism and Excretion
• Not effective orally
• Administered intravenously • Also as nasal spray(impaired milk ejection) • Not bound to plasma proteins • Catabolized by liver & kidneys • Half life = 5 minutes Role of oxytocin
Uterus • Stimulates both the frequency and force of uterine contractility particularly of the fundus segment of the uterus.
• These contractions resemble the normal
physiological contractions of uterus (contractions followed by relaxation) • Immature uterus is resistant to oxytocin.
• Contract uterine smooth muscle only at
term.
• Sensitivity increases to 8 fold in last 9
weeks and 30 times in early labor.
• Clinically oxytocin is given only when
uterine cervix is soft and dilated. Mechanism of action
• The interaction of endogenous or administered
oxytocin , with myometrial cell membrane receptor promotes the influx of ca ++ from extra cellular fluid and from S.R in to the cell , this increase in cytoplasmic calcium ,stimulates uterine contraction . Therapeutic Uses of Oxytocin 1. Induction & augmentation of labor** (slow I.V infusion)
a) Mild preeclampsia
b) Uterine inertia
c) Incomplete abortion
d) Post maturity
e) Maternal diabetes Therapeutic Uses of Oxytocin (continue)
2. Post partum uterine hemorrhage
(I.V drip) (ergometrine is often used)
3. Impaired milk ejection
One puff in each nostril 2-3 min before nursing Side Effects: 1. Maternal death due to: a) Hypertension b) Uterine rupture c) Fetal death(ischaemia) 2) Water intoxication Contraindications a) Hypersensitivity b) Prematurity c) Abnormal fetal position d) Evidence of fetal distress e) Cephalopelvic disproportion Precautions a) Multiple pregnancy b) Previous c- section c) Hypertension Ergot Alkaloids
• Ergometrine (Ergonovine)
• Methylergonovine Effects on the Uterus • Alkaloid derivatives induce TETANIC CONTRACTION of uterus without relaxation in between(not like normal physiological contractions)
• It causes contractions of uterus as a whole
i.e. fundus and cervix(tend to compress rather than to expel the fetus) Difference between oxytocin & ergots?? Ergot alkaloids( pharmacokinetics)
• Absorption ,fate and excretion
• Absorbed orally from GIT(tablets)
• Usually given I.M
• Extensively metabolized in liver.
• 90% of metabolites are excreted in bile
Clinical uses • Post partum hemorrhage (3rd stage of labor)** When to give it?
b) Hypertension b) Vasoconstriction of peripheral blood vessels ( toes & fingers) c) Gangrene • Contraindications: 1) Induction of labour a) 1st and 2nd stage of labor b) vascular disease c) Severe hepatic and renal impairment d) Severe hypertension PROSTAGLANDINS (PGE2 & PGF2α) Therapeutic uses 1. Induction of abortion (pathological)**
2. Induction of labor (fetal death in utero)
3. Postpartum hemorrhage Difference between PGS and Oxytocin:
• PGS contract uterine smooth muscle not only at
term(as with oxytocin), but throughout pregnancy.
• PGS soften the cervix; whereas oxytocin does not.
• PGS have longer duration of action than oxytocin.
• Side Effects
a) Nausea , vomiting b) Abdominal pain c) Diarrhea d) Bronchospasm (PGF2α) e) Flushing (PGE2) • Contraindications: a) Mechanical obstruction of delivery b) Fetal distress c) Predisposition to uterine rupture
• Precautions: a) Asthma b) Multiple pregnancy c) Glaucoma d) Uterine rupture Difference B/w Oxytocin and Prostaglandins
Character Oxytocin Prostaglandins
Contraction Only at term Contraction
through out pregnancy
Cervix Does not soften the soften the cervix
cervix Difference (cont’d) Character Oxytocin Prostaglandins
Duration of Shorter Longer
action uses Induce and augment Induce abortion in 2nd labour and post partum trimester of hemorrhage pregnancy.
Used as vaginal suppository for induction of labor Difference b/w Oxytocin and Ergometrine
Character Oxytocin Ergometrine
Contractions Resembles normal Tetanic contraction ; physiological doesn't resemble contractions normal physiological contractions Uses To induce &augment Only in p.partum labor. hemorrhage *Post partum hemorrhage Onset and Rapid onset Moderate onset Duration Shorter duration of Long duration of action action UTERINE RELAXANTS DRUGS PRODUCING UTERINE RELAXATION( Tocolytic Drugs ).
Action and Uses
Relax the uterus and arrest threatened abortion or delay premature labor.
1.β-ADRENOCEPTOR AGONISTS** Ritodrine, i.v. drip Selective β2 receptor agonist used specifically as a uterine relaxant. β- adrenoceptor agonists • Mechanism of action
