Carboprost is a synthetic prostaglandin analogue of PGF2α that is used to induce abortion between 13-20 weeks of pregnancy and in postpartum hemorrhage. It works by binding to FP receptors in the uterus and myometrium, causing powerful contractions that expel the products of conception. Common side effects include diarrhea, nausea, vomiting, and uterine cramping pain. It is administered as a single intramuscular injection of 250 mcg that can be repeated if needed. Carboprost has a short duration of action of 3-6 hours and is metabolized and excreted primarily in the kidneys.

1. CARBOPROST (PGF2ά)
DR ZIKRULLAH

2. Introduction
• Carboprost is a synthetic prostaglandin
analogue of PGF2ά (specifically, it is 15-
methyl-PGF2ά) with oxytocic properties.

3. Biosynthesis of PGS

4. • 20-Carbon carboxylic acids with Cyclopentane
ring
• Formed by PUFA
Prostaglandins types
Prostanoic acid
2468
10
12 14 16 18
20
PGE2
PGF2ά
COOH
PGE1

5. EICOSANOIDS
Cyclooxygenase pathway
Arachidonic Acid
Cyclooxygenase
PGG
Prostacyclin synthetase Thromboxane
synthetase
PGI2 PGH2 TXA2
PGE2 PGD2 PGF2

6. Structure

7. Chemical data
Formula C20H34O5
Mol. mass 354.48 g/mol

8. Systematic (IUPAC) name
• (5Z,9a,11a,13E,15S)-9,11,15-trihydroxy-15-
methylprosta-5,13-dien-1-oic acid

9. Preparation
• 1ml ampule containing 250 mcg of carboprost

10. Mode of Action
• G : ↑IP3, DAG, activity of this receptor
mediated by G protein which activate a
phosphatidylinositol-calcium second
messenger system initiate luteolysis in corpus
luteum
Carboprost is a uterine stimulant which results in
expulsion of the products of conception.
It is also used to induce abortion between 13-20 wk of
pregnancy.
It produces myometrial contractions responsible for
placental hemostasis.

11. Pharmakokinetics
• Metabolism :
• T ½ :
• Onset of action :
• Duration of action :
• Excretion :

12. • Metabolism of prostaglandin PG-F2 alpha
occur rapidly in most tissue but fastest in lung
by alveolar type II cells from lungs of adult
male

13. T ½ : half life of PGF2 vary from few
second to few minute .Average half
life is 1 minute.
3 to 6 hours in amniotic fluid, less
than 1 minute in blood plasma

14. • The peak plasma level of the drug is reached
about 30 minutes after injection. A successful
clinical response is expected after a single
injection in about 75% of cases. In refractory
cases, additional dosing at 15-90 minute
intervals may be beneficial. The total amount
of drug given should not exceed 2 mg (8
doses). The clinical response may be
enhanced with concomitant use of oxytocin. It
may be less effective when used in the setting
of chorioamnionitis.
Onset of action :

15. • Mainly through kidney
•Excretion

16. Type Receptor Function
PGI2 IP
•vasodilation
•inhibit platelet
aggregation
•bronchodilatation
EP1
•bronchoconstriction
•GI tract smooth
muscle contraction
EP2
•bronchodilatation
•GI tract smooth
muscle relaxation
•vasodilatation
comparison of different types of prostaglandin, prostacyclin
I2 (PGI2), prostaglandin E2 (PGE2), and prostaglandin F2α
(PGF2α).

17. PGE2
EP3
•↓ gastric acid secretion
•↑ gastric mucus secretion
•uterus contraction (when
pregnant)
•GI tract smooth muscle
contraction
•lipolysis inhibition
•↑ autonomic
neurotransmitters
•↑ platelet response to their
agonists and ↑
atherothrombosis
Unspecified
•hyperalgesia
•pyrogenic

18. PGF2α
• Act on FP receptor cause
• Uterus contraction
• Bronchocontriction

19. Uses
ABORTION
• Carboprost -15 methyl PGF2α analogue,
for midterm abortion and missed abortion.
• (It is also used for PPH.)

20. • This drug, carboprost (15-methyl-PGF2) is used to
induce second-trimester abortions
• ; not responding to conventional methods of
Methotrexate.
• The success rate is approx. 80%.
It is administered as a single 250-mcg intramuscular
injection, repeated if necessary.
• S/E- Vomiting and diarrhea.

21. FACILITATION OF LABOR
• PGE2, PGF2 , and their analogs effectively initiate and
stimulate labor,
but PGF2 is 1/10th as potent as PGE2.
• There appears to be no difference in the efficacy of
PGE2 and PGF2 when they are administered
intravenously;
• however, they may be of more use locally to promote
labor through ripening of the cervix.

22. Used in postpartum hemorrhage caused by
uterine atony not controlled by other methods.
Unlabeled use:
• Hemorrhagic Cystitis
• PID

23. Contraindications
• Hypersensitivity.
• Acute pelvic inflammatory disease.
• Patients with acute cardiac, pulmonary, renal
or hepatic disease.
• History of caesarian, major uterine surgery.
Pregnancy.

24. Precautions
• asthma
• anemia
• jaundice
• diabetes mellitus
• seizure disorders
• past uterine surgery
• Cardiopulmonary disorders,
• glaucoma,
• severe hepatic or renal dysfunction,
• labour.

25. Doses
Pregnancy termination in the 2nd trimester:
Intramuscular
• Adult: As tromethamine: 250 mcg deep IM,
repeated at 1.5 to 3.5-hr intervals depending on
uterine response. May be increased to 500 mcg if
necessary. Max: 12 mg.
Postpartum haemorrhage: Intramuscular
• Adult: As tromethamine: 250 mcg deep IM at 15-
to 90-min intervals.
• Max Dosage: 2 mg.

26. Drug interaction
• Action enhanced by prior inj of hyperosmolar
urea.
Potentially Fatal: Enhances action of oxytocin
hence both drugs should be used sequentially
and carefully monitored.

27. Side effects
Adverse Effects
• diarrhea (most common, may be sudden in
onset)
• fever
• chills
• Nausea & vomiting,
• uterine cramping pain,
• vaginal bleeding

28. Adverse Drug Reactions
• Nausea,
• vomiting,
• diarrhoea
• abdominal pain
• flushing, shivering
• headache, dizziness
• and hypotension, temporary pyrexia, dyspnoea, pulmonary
oedema.
• Potentially Fatal: Severe CVS disorders including fatal
hypotension, tachypnea, pyrexia and MI (in patients with
high risk factors) following intra-amniotic or intravaginal
admin. Convulsions and ECG changes, amniotic fluid
embolism and uterine rupture, foetal distress and rarely
foetal death during induction of labour.

29. Pregnency
• Category C: Either studies in animals have
revealed adverse effects on the foetus
(teratogenic or embryocidal or other) and
there are no controlled studies in women or
studies in women and animals are not
available. Drugs should be given only if the
potential benefit justifies the potential risk to
the foetus.

30. Pediatric Use
• Safety and effectiveness in pediatric patients
have not been established.

31. Systemic effects
• CVS :
• vasodilatation
• inotropic effect
• it also constricts many larger vein including
pulmonary vein &arteries it has little effect on BP
• Uterus :
• contraction,
• softening of cervix

32. • Bronchoconstriction
• More potent than histamine
• Asthma may be due to imbalance between
constrictor PG and dilator
Respiratory system

33. • Spasmogenic
• Increase fluid &electrolyte secretion
• Longitudinal & circular muscles of gut are
contracted
• Colic& watery diarrhoea are important side
effect due to increase propulsive activity
G.I.T.

34. .release of gonadotropins,
.prolactin,
.leuteolysis
Endocrine system

35. THANKS