Contraceptives: Oral contraceptive Steroids

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ContraceptivesOral contraceptive Steroids
By C.Adithan
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Methods of Contraception

• Direct inhibition of spermatogenesis
• Indirect inhibition of spermatogenesis
• Immunological techniques (vaccine)
• Inhibition of ovulation

• Prevention of fertilization
• Anti-zygotic drugs
• Inhibition of implantation
• use of spermicidal in vagina
• IUCD

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OCS History

• 1950 Pincus et al (progesterone prevents
  ovulation)
• 1959 1st pill appeared in USA
• 1960 mini pill (progesterone alone)
• 1970 Introduction low dose or second
  generation of OCS
• 1980 biphasic or triphasic regimens
• 1990 3rd generation OCS
• (O P has less androgenic activity,
• e.g, norgestimate 0.25mg or desogestrel 0.15 mg)

Modern pills has less than 35 mcg Oestrogen
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Inhibition of ovulation

• Oral
• Combined pill
• Sequential pill
• Phased regimen
• Mini pill
• Post-coital pill

• Injectable
• Long acting
• progest. alone
• Long acting
• progest. Oestrog.
• Implants
• Norplant

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Inhibition of ovulation

• Sequential Pills
• 16 (O) 5 (OP) 7 (DF)
• Endometrial cancer
• Mini pills
• Low dose progesterone
• Less effective
• Postcoital pills
• Need to be given within 72 h
• Mifepristone 600mg
• Low dose OE (100 mcg) norgestrel (1mg) taken
  twice
• 12 h apart 90 98 effective
• In case of failure abortion

• Phased Regimens
• Biphasic
• 10 (OP) 11 (OPP) 7 (DF)
• Triphasic
• I 6 ( E.O 30 µg Levonorg. 50 µg)
• II 5 (E.O 40 µg Levonorg. 75 µg)
• III 10 (E.O 30 µg Levonorg. 125 µg)
• Combined preparations
• 21 days (OP) 7 days (DF)
• 99 100 effective

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Combined Pills
Addition of Progesterone ensures contraceptive
effect predictable bleeding, prevent
breakthrough bleeding
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OCS Mechanism of Actions

• Gn release from pituitary
• Absence of FSH LH peaks
• Follicular development ovulation
• Thick cervical mucus
• Implantation of blastocyst in
• endometrium
• Contractions of uterus F.tubes are modified

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OCS Practical problems

• Missing a pill?
• Critical period
• Short delay
• 12 h or more late
• More than 1-2 tablets missed
• If pregnancy occurs during OCS intake
• Female with acne hirusitism
• Female with excessive menstrual loss
• If OCS is discontinued

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OCS Adverse effects
Above 35 years
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OCS Adverse effects
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OCS Drug Interactions

• A. Enzyme Inducers
• e.g., phenytoin, phenobarbitone, primidone,
  carbamazepine, rifampicin
• B. Suppression of intestinal microflora
• e.g., tetracylcine, ampicillin

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OCS Contraindications

• Thrombo-embolic, coronary cerebrovascular
  disease or history of above
• hypertension (moderate to severe)
• hyperlipidemia
• Active liver disease, hepatoma or history of
  jaundice
• Suspected / overted malignancy of genitals /
  breast
• porphyria
• Impending major surgery (post-operative
  thromboembolism)

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OCS Relative contraindications

• Diabetes
• Obesity
• Smoking
• Undiagnosed vaginal bleeding
• Uterine leiomyoma
• Mentally ill
• Above 35 years age
• Mild hypertension
• Migraine
• Gall bladder diseases

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OCS Other health benefits

• Reduced risk of
• ovarian cysts
• ovarian endometrial cancer
• benign breast diseases
• Lower incidence of ectopic pregnancy
• Less common
• Iron deficiency
• Rheumatoid arthritis

• Benefits in
• pre-menstrual tension
• dysmenorrhea
• endometriosis
• Acne hirusitism

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CENTCHROMAN

• Non-steroidal oral contraceptive (CDRI, Lucknow)
• Oestrogen antagonist
• Anti-implantation agent
• Safer free from OCS side effects menstrual cycle
  not disturbed may be lengthened in 6-10 women
• For all age group of women
• Failure rate 1 - 3
• Side effects enlargement of ovary
• C/I polycystic ovarian disease, cervical
  hyperplasia,
• renal or hepatic disease, tuberculosis
  lactating mother
• Dose 30mg tablet twice a week 30mg once a week
  till needed

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Injectable preparations

• Long acting P O once a month, i.m.
• Long acting P only higher dose, i.m. once in
  several month
• e.g., Depot medroxyprogesterone acetate (DMPA)
  150-400 mg / 3-6 months
• Norethindrone enanthate (NEE, 200 mg / 2-3
  months)
• Mech. Actions inhibit pituitray LH, suppression
  of ovulation act on
• endometrium, fallopian tube and cervcial
  secretion
• Side effects complete disruption of menstrual
  bleeding pattern
• total amenorrhea in some people
  permanent sterility
• When to start? Any time you are certain that the
  patient is not
• pregnant

WHO study combination of DMPA (25 mg)
oestradiol cypionate (5mg) has high efficacy
regular menstrual bleeding
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Implants Levonorgestrel implant

• Consists of 6 flexible silastic capsules
  containing levonorgestrel
• (36mg/capsule)
• Inserted under L.A. under the skin
• Effective for 5 years, to be replaced
  afterwards
• Mech. Actions antioestrogenic action on the
  endometrium
• cervical secretion LH peak ovulation
  suppressed
• Side effects irregular bleeding in 70 women
  few pregnancy some ectopic (1st yr), headache,
  nervousness, nausea, skin rash, acne, hirusitism,
  breast tenderness, wt. gain, enlarged ovarian
  follicles

After 1 year as effective as sterilization and
more effective than all contraceptive methods
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Best of luck for your examination