Caption

DRUGS IN PREGNANCY
MECHANISM OF ACTION
 OXYTOCICS
• Oxytocin is a nonapeptide.
• It is synthesized in the supraoptic and paraventricular
nuclei of the hypothalamus.
• By nerve axons it is transported from the hypothalamus to
the posterior pituitary where it is stored and eventually
released.
• Oxytocin has a half-life of 3–4 minutes and a duration of
action of approximately 20 minutes.
• It is rapidly metabolized and degraded by oxytocinase.
MODE OF ACTION :
• Myometrial oxytocin receptor concentration increases maximum
(100-200 fold) during labor.
• Oxytocin acts through receptor and voltage-mediated calcium
channels to initiate myometrial contractions.
• It stimulates amniotic and decidual prostaglandin production.
Bound intracellular calcium is eventually mobilized from the
sarcoplasmic reticulum to activate the contractile protein.
• The uterine contractions are physiological, i.e. causing fundal
contraction with relaxation of the cervix.
Caption
PREPARATIONS USED :
• (i) Synthetic oxytocin (Syntocinon-Sandoz or Pitocin-
Parke-Davis) is widely used. It has only got oxytocic effect
without any vasopressor action. The Syntocinon is
available in ampoules containing 5 IU/mL: Pitocin 5
IU/mL.
• (ii) Syntometrine (Sandoz)—A combination of syntocinon
5 units and ergometrine 0.5 mg.
• (iii) Desamino-oxytocin—It is not inactivated by
oxytocinase and is 50–100 times more effective than
oxytocin. It is used as buccal tablets containing 50 IU.
• (iv) Oxytocin nasal solution contains 40 units/mL.
 ERGOT DERIVATIVES
Out of many ergot derivatives, two are used extensively as
oxytocics.
• Ergometrine (Ergonovine in USA)
• Methergine (Methyl ergonovine in USA)
MODE OF ACTION :
Ergometrine acts directly on the myometrium. It excites
uterine contractions which come so frequently one after the
other with increasing intensity that the uterus passes into a
state of spasm without any relaxation in between.

CATEGORY : X
 CORTICOSTEROIDS
• BETAMETHASONE
• DEXAMETHASONE

MECHANISM OF ACTION :
• Corticosteroids accelerate type 1 and type 2
pneumocyte development, leading to structural and
biochemical changes that improve both lung
mechanics and gas exchange.
• Specific effects include induction of pulmonary beta-
receptors, which play a role in surfactant release and
absorption of alveolar fluid when stimulated .
• Induction of fetal lung antioxidant enzymes .
• Upregulation of genes for mediators of pulmonary
epithelial sodium and liquid absorption, which are
important for postnatal absorption of lung fluid
 ANTIHYPERTENSIVES IN PREGNANCY

Adrenergic Calcium ACE

receptor channel inhibitors
Sympatholy blocking Vasodilator blockers
tics agents s
•Methyldopa •Labetalol •Hydralazin •Nifedipine •Captopril
•Reserpine •Propranolol e •Nicardipine •Lisinopril
•Nitroglycer
in
•Sodium
valproate
METHYLDOPA :
Mechanism of action : central and peripheral antiadrenergic action .
Effective and safe – both mother and fetus
HYDRALAZINE :
Mechanism of action :
acts by peripheral vasodilation as it relaxes – arterial smooth
muscles,orally its weaks should be combined with methyldopa or b
blockers . Increases the cardiac output and renal blood flow .
LABETALOL :
Mechanism of action :
combined alpha and beta adrenergic blocking agent .
NIFEDIPINE :
Direct arteriolar vasodilatation by inhibition of slow inward calcium
channels in vascular smooth muscle
SODIUM NITROPRUSSIDE:
Direct vasodilator (arterial and venous) , DRUG OF LAST RESORT
NITROGLYCERIN:
Relaxes mainly the venous but also arterial smooth muscle. USE in
hypertensive crisis for a short time only
ACE inhibitors/ angiotensin- receptor blockers:
ACE inhibitors: Inhibit formation of angiotensin II from angiotensin I.
ARB–Blocks Angiotensin II receptors

ALL ANTIHYPERTENSIVES BELONG TO CATEGORY C

Calcium channel blockers (Nifedipine Nicadipine Verapamil
Nifedipine) :
blocks the entry of calcium inside the cell. It is equally effective to
MgSO4.
MAGNESIUM SULPHATE :
It acts by competetive inhibition to calcium ion either at the motor
end plate at the cell membrane reducing calcium influx Decreases
acetylcholine release and its sensitivity at the motor end plate. Direct
depressant action on the uterine muscle
INDOMETHACIN (cyclo oxygenase inhibitor):
Reduces synthesis of PGs, thereby reduces intracellular free Ca++,
activation of MLCK and uterine contractions. (PGs cause ↑ in free
intracellular Ca++ and activation of MLCK).
SULINDAC – another NSAID less placental transfer is also used .
TOCOLYTIC AGENTS :
• Preterm labor and delivery can be delayed by drugs in order to
improve the perinatal outcome.
• Short term delay of 48 hours allows the use of corticosteroids that
can reduce the perinatal mortality and serious morbidity
significantly.
• The commonly used drugs are: Betamimetics, Prostaglandin
synthetase inhibitors, Magnesium sulfate, Calcium channel blockers,
Oxytocin receptor antagonists, Nitric oxide donors and
progesterone.
Betamimetics : (Terbutaline , Ritodrine ,Isoxsuprine)
Effective for 48 hrs to allow time for steroids and antibiotics to work.
Activation of the intracellular enzymes (adenylate cyclase, cAMP,
Protein kinase), reduces intracellular free calcium (Ca++ ↓↓) and
inhibits activation of MLCK (↓↓) → Reduced interaction of actin and
myosin → smooth muscle relaxation. β (β2 ) receptor stimulation
causes smooth muscle relaxation

Oxytocin antagonists : Atosiban

Oxytocin analogue (antagonist) that blocks myometrial oxytocin
receptors. It inhibits intracellular calcium release , release of PGS and
thereby inhibits myometrial contractions.
Nitric oxide (NO) donors : Glyceryl trinitrate (GTN)
Smooth muscle relaxant
 ANTI COAGULANTS

• Heparin (unfractionated heparin)

• low-molecular- weight heparin (LMWH)
MECHANISM OF ACTION :
Inhibits action of thrombin, it also enhances the activity of antithrombin III, increases
factor Xa inhibitor
Antidote: Protamine sulfate
DOSE : 5,000–10,000 IU to be administered parenterally.
dvT and pulmonary embolism: loading dose 5,000 units IV followed by continuous
infusion of 18 units/kg/hr.
pregnancy: 5,000-10,000 SC every 12 hrs (with monitoring).
LMWH : Enoxaparin 1 mg/ kg twice daily SC, less antithrombotic effect