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Pharmacology of Drugs Acting On Uterus - MBBS

The document discusses various drugs that act on the uterus, including oxytocics like oxytocin and ergometrine that stimulate contractions, tocolytics like beta-adrenergic agonists and calcium channel blockers that relax the uterus and delay labor, and prostaglandins that can induce labor or abortions. It covers the mechanisms, pharmacokinetics, uses, and side effects of these different drug classes for stimulating or relaxing the uterus.

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Dr.U.P.Rathnakar.MD.DIH.PGDHM
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7K views23 pages

Pharmacology of Drugs Acting On Uterus - MBBS

The document discusses various drugs that act on the uterus, including oxytocics like oxytocin and ergometrine that stimulate contractions, tocolytics like beta-adrenergic agonists and calcium channel blockers that relax the uterus and delay labor, and prostaglandins that can induce labor or abortions. It covers the mechanisms, pharmacokinetics, uses, and side effects of these different drug classes for stimulating or relaxing the uterus.

Uploaded by

Dr.U.P.Rathnakar.MD.DIH.PGDHM
Copyright
© Attribution Non-Commercial (BY-NC)
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as PPT, PDF, TXT or read online on Scribd
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Drugs acting on the

uterus

Dr.U.P.Rathnakar
MD. DIH. PGDHM
K.M.C.Mangalore
Drugs Acting on the Uterus
• Introduction
• Stimulants
1. Oxytocin
2. Desamino-oxytocin
3. Ergometrine, Methyl ergometrine
4. Prostaglandins
• Tocolytics (Relaxants)
1. Adr.agonists, Ca++ blockers,
Magnesium sulfate, oxytocin antagonist,
Misc *
Drugs

• Drugs ---- Endometrium or myometrium

• Endometrium--- Estrogen or progesterone,


and antagonists
• Myometrium-
1. Indirectly acting-Symp or P.symp
[ANS drugs-non selective-other systems+]
2. Directly acting
1. Ut.stimulants (oxytocics)
2. Ut. Relaxants (Tocolytics)*
UTERINE STIMULANTS

• Post. Pit. Hormone- Oxytocin

• Ergot alkaloids- Ergometrine


(Ergonovine),
Methylergometrine

• Prostaglandins- PGE2, PGF2a, 15-Methyl


PGF2a, Misoprostol

• Miscellaneous- Alcohol, Ethacridine,


Quinine*
Oxytocin (Quick birth)
• Post Pit → Oxytocin and Vasopressin
• Synth. In hypothalumus → Transported
and stored in post. Pitutary
• Released after distension of the cervix
and vagina → birth
• Stimulation of the nipples →
breastfeeding, (Letdown or milk ejection
reflex)*
Pharmacokinetics
• Not absorbed orally
• Administerd by i.v, i.m, rarely
nasal route.
• Not bound to plasma protiens-
t1/2- 2 -5mts
• Metabolized in liver and
kidney*
Pharmacodynamics
• Acts → GPCR
• Small doses → Frequency and
force
• Large doses → Sustained
contraction
• Mammary alveoli-myoepethelial
cells → contraction
• Neurotransmitter in brain*
Ph. Actions:
• Uterus:
• Sensitivity increases as pregnancy progresses-
9 fold [early&nonpregnant-resistant]
• Receptors increase- 30 times
• Estrogen facilitates, progesterone inhibits
• Lower segment not contracted
• Breast- Milk ejection
• CVS- Hypotension
• Kidney- ADH like
• CNS*
Clinical uses of Oxytocin
• To induce, augment labor in
2. Premature rupture
3. Isoimmunization
4. Placental insufficiency
5. Toxemia, post maturity, DM

Verify fetal lung maturity, Exclude C.Is-


Position abnormalities, CPD,distress etc.
Monitor fetal HR
Look for fetal, maternal distress, ut.scar*
Induction & Augmentation
 Oxytocin DOC
 i.v. infusion pump
 Dilution-5 IU in 500ml NS/Glucose
 0.2-2ml/mt. depending on response
 Precautions→ Monitor mother and
fetus. Over stimulation →
Discontinue*
Why Oxytocin? Why not Ergometrine?

1. Short t ½
2. Normal relaxation of uterus allowed-
Good fetal oxygenation
3. Lower segment not affected-descent
free
4. Consistent augmentation in
ut.inertia*
Other uses
1. Third stage of labour, puerperium: (Post
partum hemorrhage) 5 IU i.m or i.v
infusion.
Other drugs→Ergometrine, Misoprostol
3. Breast engorgement: Nasal spray before
suckling
4. Oxytocin challenge test: To assess
placental insufficiency
• AD.Effects: Rupture ut. Fetal distress,
maternal injury*
Desamino-oxytocin

• Buccal formulation, uses same


as oxytocin, less consistent
action*
Ergometrine and Methyl ergometrine
• Amine ergot alkaloid and methyl derivative.
• Increase force, frequency, duration of
ut.contractions
• Moderate increase of dose → Basal tone
increased
• Lower segment also contracts.
• 5HT2, α Adre.agonist
• Methyl ergometrine more potent action on
uterus and less on CVS, CNS, GIT etc.*
Ad. Effects:
• Methyl ergometrine less toxic
Nausea, vomiting, rise in BP.
Decreases milk secretion
Avoided in
 Vascular disease, HTN, toxemia
 Sepsis→gangrene
 Liver and kidney disease.*
 [Safe in ob.doses]
C.I.in pregnancy & early stages of labour
Uses:

• PPH→ After anterior shoulder presentation


 Prevention → 0.2-0.3 mg i.m
 Treatment → 0.5 mg i.v.
4. Prevent uterine atony[cesarian, instrument]
5. To promote involution in multipara →
0.125mg TDS -7days
6. Diagnosis of variant angina during Coronary
angio*
•The "Four Ts" for Causes of Postpartum Hemorrhage

Approximate
•Four Ts Cause incidence (%)
Tone Atonic uterus 70

Trauma Lacerations, 20
hematomas,
inversion,
rupture
Tissue Retained tissue, 10
invasive placenta
Thrombin Coagulopathies 1
Ergometrine
Prostaglandins

• PGE2 (Dinoprostone)→ Vaginal application


→ Induce II trimester abortion, missed
abortion, ripening of cervix in near term
• Preperations-
 Misoprostol → with mifepristone for
early abortion
15-Methyl-PGF2α (Carboprost) → II
trimester abortions
Facilitate labour- Unlabelled use in
cardiac, renal disease, eclampsia*
Uterine relaxants[Tocolytics]

• Adrenergic agonists[β2]
• Ca++ channel blockers
• Magnesium sulfate
• Atosiban
• Others*
Adrenergic agonists:
• Ritodrine:
Ritodrine is a Beta-2 agonist
 ADE:
 CVS-
 Metaboloic-
 Use: To delay labour
 I.v infusion 50μg/mt
 CI: Heart disease, diabetes, on beta
blockers.
• Others: Isoxsuprine*
• Magnesium sulfate:
• Not routinely used because of toxicity.
[eclampsia-for siezures]
Ca++ channel blockers:
 Reduced Ca entry → Reduced tone
 Nifedipine → 10mg every 30 mts

Atosiban: Antagonist of oxytocin


receptors
Others: Ethyl alcohol, nitrates, Halothane
etc.*
Indications & Contraindications for
tocolytics
Ind: Delay preterm labour
CI:
More than 37 weeks gestation
Fetus >2500g
Fetus in distress
Cx dilation > 4 cm
Ruptured membrane
Toxemia,
Cardiac diseases

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