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HORMONAL
CONTRACEPTIVES
Presented by :- Dr. Indraneel Jadhav
MBBS, DGO, DNB
Consultant Gynecologist and IVF
Indira IVF, Kolhapur
PREGNANCY RATE (%)
DURING 1ST YEAR OF USE
Hatcher: Contraceptive Technology, 18th Ed
% of Women Experiencing
an Unintended Pregnancy
within the First Year of Use
% of Women
Continuing Use
at One Year
Method Typical Use Perfect
Use
No Method 85 85 42
Male Condom 15 2 53
Combined Pill and POP 8 0.3 68
Ortho Evra Patch 8 0.3 68
Vaginal Ring 8 0.3 68
DMPA 3 0.3 56
copper T IUD 0.8 0.6 78
Levonorgestrel IUS 0.1 0.1 81
Female Sterilization 0.5 0.5 100
Male Sterilization 0.15 0.10 100
HORMONAL
CONTRACEPTION
ORAL CONTRACEPTION
COMBINED, POP , SEQUENTIAL
 NON- ORAL CONTRACEPTION
INJECTABLE CONTRACEPTION
IUDs
IMPLANTS
VAGINAL RINGS
TRANSDERMAL PATCHES
ORAL
CONTRACEPTION
 1st Clinical trials of COC were described by John Charles
Rock & Goodwin Pincus with approval of marketing in
USA in 1960.
Within 5 years it was used by 30 millions women all over
the world.
At the moment , COC is used by over
100 million women worldwide.
Failure rate
• 0.3%, perfect use
• 8% typical first-year use
• Effective, safe, rapidly reversible form of contraception
COMBINED ORAL
CONTRACEPTIVES ( COC )
COMBINED ORAL
CONTRACEPTIVES ( COC )
 Commonly known as the “ Pill “
Widely Accepted & Most Effective Reversible method of
Fertility Control.
 In 1951, India was the 1st country in world to introduce COC
in National programme of Family Planning.
PILLS
ESTROGEN
 Estrogen :
2 types : - Ethinyl Estradiol ( EE )
- Mestranol ( Not used )
PHARMACOLOGY
Progestins
19-nortestosterone
Estranes Gonanes
Norethindrone
Norethindrone Acetate
Ethynodiol diacetate
Norgestrel*
Gestodene
Desogestrel
Norgestimate
17α-spironolactone
Drospirenone
17α-acetoxyprogesterone
Pregnanes
MegaceMPA
*dextro-norgestrel inactive
levo-norgestrel active
PROGESTOGENS
1 ) Norethisterone Group : ( 1st generation pills )
Moderate Androgenic property ….
Norethisterone,
Norethisterone Acetate ,
Ethiynoidal diacetate ,
Lynestrenol
2 ) Norgestrel : ( 2nd generation pills )
Strong Progestogenic & Androgenic property….
3 ) 19 – nor testosterone derivatives :( 3rd generation pills )
Anti ovulatory function by suppressing Gonadotropin…
Desogestrel,
Gestodene,
Norgestimate.
4 ) Spironolactone analogue :
Antiandrogenic & Anti mineralocorticoid …
Drosperinone ( DRSP )
PROGESTOGENS
COMPARISON OF PROGESTIN
Progestin Anti-
estrogenic
Androgenic Anti-
androgenic
Anti-
mineralocorticoid
Progesterone - - + +
Older progestins:
MPA
Norethisterone
Levonorgestrel
-
+
+
+
+
+
-
-
-
-
-
-
Newer progestins:
Desogestrel
Cyproterone acetate
-
-
-
-
-
+
-
-
Drospirenone - - + +
Metabolic Effects of
Estrogen and Progestin
Estrogen Progestin
Protein  Globulin synthesis*  SHBG
Lipids
HDL cholesterol  
LDL cholesterol  
Total cholesterol  
Triglycerides  
* Including many clotting factors, angiotensinogen, and SHBG
TYPES OF COC
PATTERNS OF PILL USE
• Monthly cycling 21/7
• Multiphasic Preparations
• Alters the dosage of both the estrogen and progestin
components periodically throughout the pill-taking schedule
• Reduction in pill-free intervals
• Using a 4-day pill-free interval is associated with greater
ovarian suppression.
• Extended cycle regimens (bicycling, tricycling)
• 42 – 84 active followed by 7 inactive pills
• Seasonale, Seasonique
• Continuous use
MONOPHASIC
 Contains Estrogen & Progesterone in same amount in
Each pill .
 Divided in 2 subgroups :
- Low dose pills : EE 30 – 35 microgm
- Very low dose pills : EE 15 – 25 microgm
Ovral –L; Mala-D; Mala-N LNG 0.15 mg /EE 30 mcg
Novelon Desogesterol 0.15 mg
/EE 30 mcg
Femilon Desogesterol 0.15 mg
/EE 20 mcg
Elogen Desogesterol 0.15 mg
/EE 20 mcg
Yasmin 3 mg DRSP/ EE 30 mcg
MULTIPHASIC
 Contains low or variable amounts of Progesterone in
2 ( biphasic ) or 3 ( triphasic ) phases of cycles.
 Biphasic :
constant EE – 35 microgm
progestogens : low in first 10 days
higher in next 11 days .
NOT POPULAR – MORE FAILURE RATE .
NOT AVAILABLE IN INDIA …
 Triphasic : Triquilar –
- 0.03 EE +0.5mg l-norgestrel (1 - 6)
- 0.03 EE +0.75mg l-norgestrel (7-11)
- 0.03 EE +0.125mg l-norgestrel (12 - 21)
Total monthly intake – 0.68mg EE +1.92mg progesterone
• Adv. – high efficacy rates
- few side effects
- less break through bleeding
- does not affect s.cholesterol & LIPIDS
• Disadv. – high pregnancy rates if errors in pill intake .
MULTIPHASIC
GnRH triggers release of
FSH & LH
FSH & LH trigger ovulation
Estrogen & progesterone in
hormonal contraceptives
inhibit LH, FSH, and GnRH
secretion,
preventing ovulation

Progesterone:
•thickens cervical mucus to prevent
passage of sperm into the uterus
•changes uterine lining to inhibit implantation

MECHANISM OF ACTION:
MECHANISM OF ACTION
• Mostly a progestin effect
• Block LH surge, inhibiting ovulation. (breakthrough ovulation
rate 2-8% depending on EE dose)
• Thicken cervical mucus
• Inhibit capacitation of sperm
• Slow tubal motility
• Distrupt transport of fertilized ovum
• Endometrial changes (atrophy, underlying vascular function and
structure and alter the metalloprotein content)
• Estrogen (ethinyl estradiol or mestranol)
• Cycle control
• acts to inhibit follicular growth by decreasing FSH
SELECTION OF THE PATIENT
 Detail history ( headache , migraine , etc…)
 Thorough general examination
( Breast , blood pressure… )
 Pelvic examination to exclude cervical pathology.
 Cervical cytology
 Rule out any other contraindications.
CHECKLIST FOR
PRESCRIBING COC…
Last menstrual period, rule out pregnancy
Less than 6 months postpartum & lactating?
Age, Cigarette smoking, h/o migraine
Known case of diabetes or hypertension
History of stroke, MI or thrombosis
h/o jaundice/ liver disease
h/o breast/ genital tract malignancies
h/o drug intake: Antitubercular, antiepileptic
ADMINISTRATION
New User :
- 1st day of Cycle .
- Daily 1 tab. Preferably at night for consecutive 21 days.
- Continued for 21 days and then 7 days break ( with iron
tablets ) .
- Next pack of Pill should be started on 8th day ,
IRRESPECTIVE OF BLEEDING ( same day of the week , pill
finished ).
- Simple Regimen of “ 3 WEEKS ON & 1 WEEK OFF “
- No break between packs.
 Can start pill up to 5 days of bleeding with extra precaution
with condom for next 7 days.
PILL INITIATION
METHODS
• Quick-start
• Day of visit
• Reasonably sure not pregnant
• 7 days back-up
• Remind that menses may be delayed or irregular
• More successful at getting women started on the
pills.
• First-day start
• In regularly ovulating, normal menses
• Sunday start
• Back up needed for 7 days.
• Not usually recommended.
PILL INITIATION
METHODS
• Lactating Women –
Combined pills after 6 months
• Non Lactating Women –
Combined oral pills after 3 to 6 weeks or after menstruation
• 1st / 2nd Trimester abortion –
during first 7 days.
• Amenorrhea
At any time after excluding pregnancy +
barrier method for 7 days.
1 missed –
Take 2 tablets next day .
2 or 3 missed –
Take 2 tablets on two consecutive days and continue the rest of
the pack.
+Another Contraceptive for 1 week.
MISSED
PILLS
SEASONALE
Available since 2003
150µg of LNG + 30µg of EE
Only Active Pills taken continuously for 84 days, then break
for 7 days.
Fewer periods (4 in a year)
Pearl index- 0.78
Breakthrough bleeding/ spotting – First few cycles
FOLLOW UP …
 Examined after 3 months , then after
6 months and then yearly .
 Ask for any symptoms…
 Examination for breast , pelvis, BP & weight & cervical
cytology.
ADVANTAGES…
• Prevention of pregnancy
India - MMR 1per 57 i.e. 400 in 1,00,000
2/5th of these deaths can be prevented by use of OCs
• Cyclical Stabilisation
Great social advantage. Withdrawl
bleeding is predictable & postponed safely by taking
more low dose pills contineously .
• Cure of Menstrual Disorders
Dysmenorrhoea & Ovulation pain –
By inhibiting ovulation & production of PG .
Menorrhagia & Metrorrhagia –
Norgestrel High dose oral pills more useful.
Lessens PMT.
• Protection against Cancer
a) Endometrial cancer- Reduction by 50 %
effect persists for 15 yrs.
b) Ovarian Cancer – Reduction by 40 %
effect persists for 10 yrs.
c) Choriocarcinoma – Indirectly prevention by preventing
pregnancy.
ADVANTAGES…
• Protection against benign tumors
1) Fibrocystic and Fibroadenomatous disease
2) Ovarion Functional Cysts
1) Follicular Cyst – 50 %
2) Corpus Luteum Cyst – 80 %
3) Fibroid Uterus - Reduction by 30%
Low Dose OC’s reduce fibroid ( WHO 1996)
ADVANTAGES…
• Protection against diseases
1) Ectopic Pregnancy
2) PID
3) Anemia and Malnutrition
4) Endometriosis
5) Acne and Hirsutism
6) DUB
7) Osteoporosis
• Simplicity and Attractiveness
• No Affection on Future fertility ( 3 months )
ADVANTAGES…
EMERGENCY
CONTRACEPTION…
1) Yuzpe regimen –
0.1mg EE + 1 mg dl-Norgestrel
1st dose Within 72 Hrs of Contact
Repeated after 12 Hrs.
2) Ovral
1st dose 2 tablets within 72 hrs.
2nd dose 2 tablets after 12 hrs.
3) Overal – L
1ST dose 4 tablets within 72 hrs.
2nd dose 4 tablets after 12 hrs.
NEW ORAL CONTRACEPTION
• Newer progestogens –
Dienogest, Nomegestrel, Drospirenone
• Antiandrogenic activity with additional anti
mineralocorticoid activity of Drospirenone
• Significant reduction in the dosage
• Estradiol (E2) is used as estrogen instead of Ethinyl
Estradiol (EE)
Trials
• E2/Drospirenone & E2/Nomegestrol –
Monophasic & Triphasic formulation
• E2/Dienogest –
Quadriphasic formulation
• Estetrol (E4) –
• 18 times less potent than EE
• Fewer side effects
• Possibility of E4 protective against breast cancer is proposed
• Now classified as SERM
• Selective progesterone receptor blocker (SPRM)
block receptors in ovary, inhibit LH
a. Mifepristone : 5mg daily or 25mg weekly effective contraception
(Phase II Trial)
b. Ulipristal : daily pill
NEW ORAL CONTRACEPTION
Femcon Fe
(norethindrone 0.4mg & ethinyl estradiol 35mcg
& ferrous fumarate tablets)
Chewable birth control
Spearmint flavored
LoEstrin 24 Fe
(Norethindrone acetate 1mg & Ethinyl Estradiol 20mcg)
24 hormone days with 4 placebo days
NEWER PILLS
NEWER EC’S
Acts by delaying ovulation
Selective progesterone receptor modulator
a. Mifepristone 10mg
b. Ulipristal
COX 2 Inhibitors
a. Meloxicam - prevents rupture of dominant follicle , in
combination with LNG has better efficacy
b. Rofecoxib - delay in follicle rupture
MINOR SIDE EFFECTS…
1. Nausea, Vomiting and Lack of appetite
2. Break through bleeding (BTB)
3. Menorrhagia and irregular bleeding
4. Oligomenorrhoea and Amenorrhoea
5. Breast changes –
Heaviness and Tenderness
6. Vaginal Discharge –
Cervix -erosion, dysplasia causes leucorrhoea
7. Chloasma
8. Weight Gain
9. Psychosexual Trouble –
Depression, Loss of Libido
10. Others - Leg Cramps, Dimness of Vision
MAJOR SIDE EFFECTS…
• Cardiovascular Diseases
1) MI – Increased Risk in heavy smokers
2) Ischaemic Stroke - 1.5 times more
3) Haemorrhagic Stroke – double risk
4) Venous Thromboembolism – Risk increases with age,
recent surgery and thrombophilia
• Hypertension - In women more than 35 Yrs.
• Carcinogenecity
1) Breast Cancer
2) Cervical Cancer
INTERACTION WITH
DRUGS…
Contraception failure Increase COC activity Clearance decreased
Carbamazepine Acetaminophen Amitriptyline
Griseofulvin Erythromycin Caffeine
Oxcarbazepine Fluoxetine Cyclosporine
Phenobarbitol Fluconazole Diazepam
Phenytoin Fluvoxamine Imipramine
Primidone Grapefruit juice Phenytoin
Rifampin Nefazadone Selegiline
Ritonavir Vitamin C Theophylline
St. John’s Wort
Topiramate
ABSOLUTE
CONTRAINDICATIONS…
(WHO CATEGORY IV)
1. Migraine, with focal Neurological Symptoms
2. Pregnancy and breast feeding ( 6 Months)
3. Severe Hypertension
4. Complicated valvular heart disease
5. D.M. with vascular complications
6. Active hepatitis, liver tumors
7. Major Surgery
8. Prolonged Immobilization .
INDICATIONS OF WITHDRAWAL
PROGESTIN ONLY
CONTRACEPTIVES
Oral pill 1973
Injectable suspension
Intramuscular 1968 (1992 U.S.)
Subcutaneous 2005
Subdermal Implant
6 LNG 1990
2 LNG 1996
1 ENG 2001 (2006 U.S)
Intrauterine System (LNG) 2002
MINI PILLS
PREPARATIONS
INDICATIONS :
Age > 40 Yrs.
Lactating Women.
Norethindrone 0.350 mg Micronor/noriday
Levonorgesterol 0.075 mg Neogest
Norgesterol 0.030 mg Microval/norgeston
Ethynodiol diacetate 0.500 mg Femulen
Desogesterol 0.075 mg Cerazette/zerogen
MECHANISM OF ACTION
• Ovulation inhibition by decreased GnRH pulse
frequency.
• Suppression of midcycle LH and FSH surge
• Thickened and decreased cervical mucus
• Endometrial changes (atrophic endometrium)
MINI PILLS
Schedule
• 1st day of M.C. and a backup method for 7 days
• 6 wks after delivery – no backup method
• Missed Tablet – Backup method for 48 Hrs.
• Failure Rate - 3- 10 %
Lactating Women – 0.5 %
Advantages
Can be used above 16 yrs of age, Smokers & obesity
Best in DM, CVS Diseases & SLE
Disadvantages
Irregular Bleeding, Acne, Mastalgia, Amenorrhoea
NON ORAL
CONTRACEPTION
1) Progesterone
DMPA – 150 mg Depoprovera IM
- Repeat every 3 Months
NET-EN – 200 mg Norethisterone enanthate
- Repeat every 2 months
2) Combined
Cyclofem – DMPA 25 + Oestradiol cypionate 5 mg
Mesigna - NET-EN 50 + Oestradiol Valerate 5 mg
INJECTABLE CONTRACEPTIVES
• Dose Schedule
5 to 7 days of menstruation
Post- abortal – Immediate
Post- delivery – 6 Wks
• Technique : DMPA IM in arms
NET-EN in buttocks
( Needs warming )
INJECTABLE CONTRACEPTIVES
DEPO-SUBQ PROVERA 104
 New formulation for subQ injection
 30% lower dose (104 mg vs. 150 mg)
 Rapid onset of action
 Same effectiveness, same length of protection (>3 months)
 Approved by USFDA (2005) and UK
 Potential for home- and self-injection
 Available for roll-out in 2011; Acceptability studies to begin in mid-2010
Uniject:
• Single dose, single package
• Prefilled, sterile, non-reusable
• Short needles for subQ injection (easier use by non-clinical
personnel/CHWs)
• Compact; easy to use and store
Mode of Action
• Inhibits ovulation
• Cervical mucus thickening
• Endometrial alteration
Eligibility criteria
Adolescents > 16 yrs of Age
Nulliparous
Obese / Thin
Smokers
6 Wks post delivery
Post Abortal
INJECTABLE CONTRACEPTIVES
CONTRAINDICATIONS
Absolute
Pregnancy
Unexplained genital
bleeding
Severe coagulation
disorders
Previous sex steroid
induced liver adenoma
Relative
Liver disease
Severe cardiovascular
disease
Severe depression
Difficulty with injections
Advantages
• Easy & Convinient to use
• Safe, no serious health effects
• Free from estrogen related
problems
• Reduces menstrual flow &
prevents anemia
• Suitable for lactating women
• Reduces risk- PID & vaginal
candidiasis
• Protects against endometrial
cancer for 8 years after
discontinuation
Disadvantages
• Irregular menstrual bleeding
• Weight gain
• Impaired glucose tolerance
• Affection of fertility- delay
• Risk of carcimona insitu &
invasive cervical carcinoma in
HIV
• Bone density changes
• Headache, weight gain,
dizziness, abdominal pain,
anxiety
HORMONE RELEASING IUD
 Progestasert
 Levonorgestrel IUD 20 – LNG 20
 T Shaped
 Hormonal capsules in the vertical rod.
 Maintains high local level of progesterone and low
estrogen
Progesterone IUD
38 mg of progesterone
65 mcg of Progesterone / Day
Reduces Menstrual loss
Disadvantage
Costly
1 Yr. Life
Insertion may require LA / Sedation
HORMONE RELEASING IUD
MIRENA
40 – 60 mg of LNG on stem.
Release 20 mcg / Day
Life 5 Years
Failure Rate 0.1 to 0.4 %
Difficult Insertion due to greater thickness
Advantages –
Contraception
DUB
IMPLANTS
• Sub dermal drug delivery system
• ADV: - long acting , reversible, progesterone only
• TYPES OF IMPLANTS
1. Norplant – has 6 rods
2. Jadella & Norplant 2 – has 2 rods
3. Implanon – has 1 rod
UNIPLANT
• Single rod implant
• Nomegestrol 38 mg.
• Releases 100 microgm / day.
• For 1 year.
NORPLANT
• 6 Silastic rod – 3.4 mm x 2.4 mm
• 36 mg LNG
• Daily release 50 – 80 mcg for 1st yr.
30 – 35 mcg over next 5 yrs.
• Life 5 Yrs.
• Insertion –
Day 1 – 7 of M.C.
Immediately after abortion
6 Wks after delivery
TECHNIQUE
 Arm / Forearm under the skin
 Under L.A
 Small incision made
 6 rods inserted in fan shaped manner
 Special trocar used for insertion
 Effective within 24 Hrs.
 Removal after 5 Yrs. under LA
Mechanism
• Suppression of Hypothalamic and pituitary hormones and prevents
ovulation
• Depresses endometrial growth
• Cervical Mucus thickening
Eligibility -
Women of all ages
Women who do not want pregnancy for several years
Disadvantages
1) Trained person required for insertion and removal
2) Irregular bleeding
3) Infection
4) Hematoma
5) Removal may be difficult
NORPLANT
JADELLE / NOR PLANT II
• 2 Solid Silastic rod
• 44 mm x 2 mm
• Inserted on medial aspect of upper arm
• 70 mg of LNG – Release 30 to 35 mcg daily
• Life 5 Years
Norplant
First month- 85µg
1year- 35µg
2year- 30µg
Jadelle
First month- 100µg
1year- 40µg
2year- 30µg
IMPLANON
• Long acting single rod subdermal implant
• Length – 4 cm ,2mm diameter
• DOSAGE: 68mg of crystalline etonorgestrel in ethylene
vinyl acetate copolymer
• DURATION : 3 years
ADVANTAGES :
 Long acting sustainable contraceptive
 Low systemic side effects
 Can be used by lactating mothers
DISADVANTAGES :
 Ectopic pregnancy- 1.3%
 Local infection
 EXPENSIVE
 Has to insert & remove the capsules
IMPLANON
BIODEGRADABLE
• Cipronor ( Single Capsule) – IMPLANTS :
- LNG 26 mg
- begins to disappear after 12 months.
• INJECTABLE :
- Microsphere of 0.06 – 0.1 mm diameter with Norethindrone with or
without EE.
- Given over Gluteal muscle.
- Once injected , can’t be removed.
How they work :
• Hormones diffuse continuously from a reservoir within the
ring into the bloodstream absorbed through vaginal
epithelium
• Combined vaginal rings prevents ovulation, thicken the
cervical mucous & suppress the endometrial growth
Side effects :
leucorrhoea, vaginal discomfort, vaginitis, foreign body
sensation, coital problems, expulsion
CONTRACEPTIVE VAGINAL RINGS
Combined progestin & estrogen rings
Nestorone ring
(Nestorone 150-200mcg + EE 15-20mcg/day)
Effective 12 months (Phase III Trial)
Emergency contraception
Nuva ring
(Etonogetrel 120mcg + EE 15mcg/day)
Use for 3week & 1 ring-free week
CONTRACEPTIVE VAGINAL RINGS
Progesterone only rings (Progering)
Less effective
Preferred in lactating
Progesterone 10mg/day - Effective up to 4 months
Nestorone releasing ring - Effective up to 1 year
Ulipristal in vaginal ring – Trial on going
CONTRACEPTIVE VAGINAL RINGS
• Nuva ring releases 15µg ethinyl estradiol & 120µg
etonogestrel/day
• Circulating hormones reach target within 24hrs &
remains stable for 24hrs
• Requires insertion of new ring every 4weeks
• If ring is removed & not replaced within 3hrs-backup
contraception for 7days reqiured.
NUVA RING
Failure rate 0.3%
TRANSDERMAL CONTRACEPTION
How they work
• Patches release estrogen & progestin through the skin, prevents
ovulation, thickening the cervical mucus, suppressing endometrial
growth
• User replaces patch weekly for 3 weeks & 1 patch free week
3 layers :
a. Outer - polyester protective layer
b. Middle - medicated adhesive layer
c. Inner - polyester release liner
 Ortho Evra
 (EE 20mcg + Norelgestromin 150mcg / day)
 Gestadone patch
 (EE 18mcg + Gestadone 50mcg/ day)
TRANSDERMAL CONTRACEPTION
Spray on contraceptive (Nestorone)
Single daily progestin only spray-on*
Absorbed into the skin & diffuses into the blood stream
Inhibits ovulation
The Metered Dose Transdermal System - spray*
(*Phase 1 trial …..Australia )
Gel (Nestrone)
Single daily application
CENTCHROMAN ( SAHELI )
• Ormeloxifene .
• research product of CDRI , Lucknow
• Non steroidal , potent anti estrogenic , weak estrogenic.
• Prevent implantation of fertilized ovum .
• Orally 30 mg twice weekly for first 3 months then once a
week.
• Avoided in PCOD, liver , kidney disease.
CENTCHROMAN ( SAHELI )
MALE HORMONAL METHODS
New male pill
• Desogestrel + Testosterone
• Blocks the production of sperm - maintaining male
characteristics & libido
• Daily pill
• 100% effective and completely reversible in preliminary
clinical trials
• In clinical trials, all of the participants’ sperm counts dropped
to zero, which means that the male pill would be more
effective than the condom and even the female pill.
CatSper blocker
• Sperm rely on calcium ions in sperm tail for mobility &
fertilization
• Humans -ion-channel gene - CatSper.
• Blocking CatSper action - effective form of birth control
• Men or women could take this potential CatSper “blocker”
• It acts ”wherever sperm are present”
• Active only in fully developed sperm
MALE HORMONAL METHODS
GENDARUSSA
• First non hormonal male contraceptive pills.
• Developed by Indonesia.
• Active ingredient in Gendarussa disrupts an enzyme in
the sperm head, which weakens the ability of the sperm
to penetrate the ovum.
• The effect is short term and reversible – having no effect
on male hormones.
• Still under clinical trials…
The Male Patch (Adjudin)
Adjudin (2,4-dichlorobenzyl- 1H-indazole-3-carbohydrazide)
Non-hormonal male contraceptive
Acts by blocking maturation of sperm in the testes
No effect on testosterone production
• Normal spermatogenesis returned in 95% within 210 days
after the drug had been discontinued
• The oral dose effective for contraception - high : causing
side effects in muscles & liver
Patch or implant – Avoids 1st pass metabolism
MALE TRANSDERMAL PATCH
REFERENCES
• S Rowlands. New technologies in contraception. BJOG 2009; 116:230-239.
• Allen RH, Goldberg AB, Grimes DA. Expanding access to intrauterine contraception.
American Journal of Obstetrics and Gynecology 2009;201(5):456-61.
• Grimes DA, Lopez LM, Schulz KF, Immediate post-partum insertion of intrauterine devices
Review, published in The Cochrane Library2010, Issue 5.
• WHO, Family Planning A GLOBAL HANDBOOK FOR PROVIDERS Update 2011.
• “Guidelines for administration of emergency contraceptive pills by medical officers,”
Research Studies and Standard Division, Department of Family Welfare, Government of
India, June 2009.
• The essentials of Contraceptive Technology, a handbook for clinic staff, John Hopkins
Population Information Program, 2010.

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Hormonal contraceptives

  • 1. HORMONAL CONTRACEPTIVES Presented by :- Dr. Indraneel Jadhav MBBS, DGO, DNB Consultant Gynecologist and IVF Indira IVF, Kolhapur
  • 2. PREGNANCY RATE (%) DURING 1ST YEAR OF USE Hatcher: Contraceptive Technology, 18th Ed % of Women Experiencing an Unintended Pregnancy within the First Year of Use % of Women Continuing Use at One Year Method Typical Use Perfect Use No Method 85 85 42 Male Condom 15 2 53 Combined Pill and POP 8 0.3 68 Ortho Evra Patch 8 0.3 68 Vaginal Ring 8 0.3 68 DMPA 3 0.3 56 copper T IUD 0.8 0.6 78 Levonorgestrel IUS 0.1 0.1 81 Female Sterilization 0.5 0.5 100 Male Sterilization 0.15 0.10 100
  • 3. HORMONAL CONTRACEPTION ORAL CONTRACEPTION COMBINED, POP , SEQUENTIAL  NON- ORAL CONTRACEPTION INJECTABLE CONTRACEPTION IUDs IMPLANTS VAGINAL RINGS TRANSDERMAL PATCHES
  • 5.  1st Clinical trials of COC were described by John Charles Rock & Goodwin Pincus with approval of marketing in USA in 1960. Within 5 years it was used by 30 millions women all over the world. At the moment , COC is used by over 100 million women worldwide. Failure rate • 0.3%, perfect use • 8% typical first-year use • Effective, safe, rapidly reversible form of contraception COMBINED ORAL CONTRACEPTIVES ( COC )
  • 6. COMBINED ORAL CONTRACEPTIVES ( COC )  Commonly known as the “ Pill “ Widely Accepted & Most Effective Reversible method of Fertility Control.  In 1951, India was the 1st country in world to introduce COC in National programme of Family Planning.
  • 8. ESTROGEN  Estrogen : 2 types : - Ethinyl Estradiol ( EE ) - Mestranol ( Not used )
  • 9. PHARMACOLOGY Progestins 19-nortestosterone Estranes Gonanes Norethindrone Norethindrone Acetate Ethynodiol diacetate Norgestrel* Gestodene Desogestrel Norgestimate 17α-spironolactone Drospirenone 17α-acetoxyprogesterone Pregnanes MegaceMPA *dextro-norgestrel inactive levo-norgestrel active
  • 10. PROGESTOGENS 1 ) Norethisterone Group : ( 1st generation pills ) Moderate Androgenic property …. Norethisterone, Norethisterone Acetate , Ethiynoidal diacetate , Lynestrenol 2 ) Norgestrel : ( 2nd generation pills ) Strong Progestogenic & Androgenic property….
  • 11. 3 ) 19 – nor testosterone derivatives :( 3rd generation pills ) Anti ovulatory function by suppressing Gonadotropin… Desogestrel, Gestodene, Norgestimate. 4 ) Spironolactone analogue : Antiandrogenic & Anti mineralocorticoid … Drosperinone ( DRSP ) PROGESTOGENS
  • 12. COMPARISON OF PROGESTIN Progestin Anti- estrogenic Androgenic Anti- androgenic Anti- mineralocorticoid Progesterone - - + + Older progestins: MPA Norethisterone Levonorgestrel - + + + + + - - - - - - Newer progestins: Desogestrel Cyproterone acetate - - - - - + - - Drospirenone - - + +
  • 13. Metabolic Effects of Estrogen and Progestin Estrogen Progestin Protein  Globulin synthesis*  SHBG Lipids HDL cholesterol   LDL cholesterol   Total cholesterol   Triglycerides   * Including many clotting factors, angiotensinogen, and SHBG
  • 15. PATTERNS OF PILL USE • Monthly cycling 21/7 • Multiphasic Preparations • Alters the dosage of both the estrogen and progestin components periodically throughout the pill-taking schedule • Reduction in pill-free intervals • Using a 4-day pill-free interval is associated with greater ovarian suppression. • Extended cycle regimens (bicycling, tricycling) • 42 – 84 active followed by 7 inactive pills • Seasonale, Seasonique • Continuous use
  • 16. MONOPHASIC  Contains Estrogen & Progesterone in same amount in Each pill .  Divided in 2 subgroups : - Low dose pills : EE 30 – 35 microgm - Very low dose pills : EE 15 – 25 microgm Ovral –L; Mala-D; Mala-N LNG 0.15 mg /EE 30 mcg Novelon Desogesterol 0.15 mg /EE 30 mcg Femilon Desogesterol 0.15 mg /EE 20 mcg Elogen Desogesterol 0.15 mg /EE 20 mcg Yasmin 3 mg DRSP/ EE 30 mcg
  • 17. MULTIPHASIC  Contains low or variable amounts of Progesterone in 2 ( biphasic ) or 3 ( triphasic ) phases of cycles.  Biphasic : constant EE – 35 microgm progestogens : low in first 10 days higher in next 11 days . NOT POPULAR – MORE FAILURE RATE . NOT AVAILABLE IN INDIA …
  • 18.  Triphasic : Triquilar – - 0.03 EE +0.5mg l-norgestrel (1 - 6) - 0.03 EE +0.75mg l-norgestrel (7-11) - 0.03 EE +0.125mg l-norgestrel (12 - 21) Total monthly intake – 0.68mg EE +1.92mg progesterone • Adv. – high efficacy rates - few side effects - less break through bleeding - does not affect s.cholesterol & LIPIDS • Disadv. – high pregnancy rates if errors in pill intake . MULTIPHASIC
  • 19. GnRH triggers release of FSH & LH FSH & LH trigger ovulation Estrogen & progesterone in hormonal contraceptives inhibit LH, FSH, and GnRH secretion, preventing ovulation  Progesterone: •thickens cervical mucus to prevent passage of sperm into the uterus •changes uterine lining to inhibit implantation  MECHANISM OF ACTION:
  • 20. MECHANISM OF ACTION • Mostly a progestin effect • Block LH surge, inhibiting ovulation. (breakthrough ovulation rate 2-8% depending on EE dose) • Thicken cervical mucus • Inhibit capacitation of sperm • Slow tubal motility • Distrupt transport of fertilized ovum • Endometrial changes (atrophy, underlying vascular function and structure and alter the metalloprotein content) • Estrogen (ethinyl estradiol or mestranol) • Cycle control • acts to inhibit follicular growth by decreasing FSH
  • 21. SELECTION OF THE PATIENT  Detail history ( headache , migraine , etc…)  Thorough general examination ( Breast , blood pressure… )  Pelvic examination to exclude cervical pathology.  Cervical cytology  Rule out any other contraindications.
  • 22. CHECKLIST FOR PRESCRIBING COC… Last menstrual period, rule out pregnancy Less than 6 months postpartum & lactating? Age, Cigarette smoking, h/o migraine Known case of diabetes or hypertension History of stroke, MI or thrombosis h/o jaundice/ liver disease h/o breast/ genital tract malignancies h/o drug intake: Antitubercular, antiepileptic
  • 23. ADMINISTRATION New User : - 1st day of Cycle . - Daily 1 tab. Preferably at night for consecutive 21 days. - Continued for 21 days and then 7 days break ( with iron tablets ) . - Next pack of Pill should be started on 8th day , IRRESPECTIVE OF BLEEDING ( same day of the week , pill finished ). - Simple Regimen of “ 3 WEEKS ON & 1 WEEK OFF “ - No break between packs.  Can start pill up to 5 days of bleeding with extra precaution with condom for next 7 days.
  • 24. PILL INITIATION METHODS • Quick-start • Day of visit • Reasonably sure not pregnant • 7 days back-up • Remind that menses may be delayed or irregular • More successful at getting women started on the pills. • First-day start • In regularly ovulating, normal menses • Sunday start • Back up needed for 7 days. • Not usually recommended.
  • 25. PILL INITIATION METHODS • Lactating Women – Combined pills after 6 months • Non Lactating Women – Combined oral pills after 3 to 6 weeks or after menstruation • 1st / 2nd Trimester abortion – during first 7 days. • Amenorrhea At any time after excluding pregnancy + barrier method for 7 days.
  • 26. 1 missed – Take 2 tablets next day . 2 or 3 missed – Take 2 tablets on two consecutive days and continue the rest of the pack. +Another Contraceptive for 1 week. MISSED PILLS
  • 27. SEASONALE Available since 2003 150µg of LNG + 30µg of EE Only Active Pills taken continuously for 84 days, then break for 7 days. Fewer periods (4 in a year) Pearl index- 0.78 Breakthrough bleeding/ spotting – First few cycles
  • 28. FOLLOW UP …  Examined after 3 months , then after 6 months and then yearly .  Ask for any symptoms…  Examination for breast , pelvis, BP & weight & cervical cytology.
  • 29. ADVANTAGES… • Prevention of pregnancy India - MMR 1per 57 i.e. 400 in 1,00,000 2/5th of these deaths can be prevented by use of OCs • Cyclical Stabilisation Great social advantage. Withdrawl bleeding is predictable & postponed safely by taking more low dose pills contineously .
  • 30. • Cure of Menstrual Disorders Dysmenorrhoea & Ovulation pain – By inhibiting ovulation & production of PG . Menorrhagia & Metrorrhagia – Norgestrel High dose oral pills more useful. Lessens PMT. • Protection against Cancer a) Endometrial cancer- Reduction by 50 % effect persists for 15 yrs. b) Ovarian Cancer – Reduction by 40 % effect persists for 10 yrs. c) Choriocarcinoma – Indirectly prevention by preventing pregnancy. ADVANTAGES…
  • 31. • Protection against benign tumors 1) Fibrocystic and Fibroadenomatous disease 2) Ovarion Functional Cysts 1) Follicular Cyst – 50 % 2) Corpus Luteum Cyst – 80 % 3) Fibroid Uterus - Reduction by 30% Low Dose OC’s reduce fibroid ( WHO 1996) ADVANTAGES…
  • 32. • Protection against diseases 1) Ectopic Pregnancy 2) PID 3) Anemia and Malnutrition 4) Endometriosis 5) Acne and Hirsutism 6) DUB 7) Osteoporosis • Simplicity and Attractiveness • No Affection on Future fertility ( 3 months ) ADVANTAGES…
  • 33. EMERGENCY CONTRACEPTION… 1) Yuzpe regimen – 0.1mg EE + 1 mg dl-Norgestrel 1st dose Within 72 Hrs of Contact Repeated after 12 Hrs. 2) Ovral 1st dose 2 tablets within 72 hrs. 2nd dose 2 tablets after 12 hrs. 3) Overal – L 1ST dose 4 tablets within 72 hrs. 2nd dose 4 tablets after 12 hrs.
  • 34. NEW ORAL CONTRACEPTION • Newer progestogens – Dienogest, Nomegestrel, Drospirenone • Antiandrogenic activity with additional anti mineralocorticoid activity of Drospirenone • Significant reduction in the dosage • Estradiol (E2) is used as estrogen instead of Ethinyl Estradiol (EE) Trials • E2/Drospirenone & E2/Nomegestrol – Monophasic & Triphasic formulation • E2/Dienogest – Quadriphasic formulation
  • 35. • Estetrol (E4) – • 18 times less potent than EE • Fewer side effects • Possibility of E4 protective against breast cancer is proposed • Now classified as SERM • Selective progesterone receptor blocker (SPRM) block receptors in ovary, inhibit LH a. Mifepristone : 5mg daily or 25mg weekly effective contraception (Phase II Trial) b. Ulipristal : daily pill NEW ORAL CONTRACEPTION
  • 36. Femcon Fe (norethindrone 0.4mg & ethinyl estradiol 35mcg & ferrous fumarate tablets) Chewable birth control Spearmint flavored LoEstrin 24 Fe (Norethindrone acetate 1mg & Ethinyl Estradiol 20mcg) 24 hormone days with 4 placebo days NEWER PILLS
  • 37. NEWER EC’S Acts by delaying ovulation Selective progesterone receptor modulator a. Mifepristone 10mg b. Ulipristal COX 2 Inhibitors a. Meloxicam - prevents rupture of dominant follicle , in combination with LNG has better efficacy b. Rofecoxib - delay in follicle rupture
  • 38. MINOR SIDE EFFECTS… 1. Nausea, Vomiting and Lack of appetite 2. Break through bleeding (BTB) 3. Menorrhagia and irregular bleeding 4. Oligomenorrhoea and Amenorrhoea 5. Breast changes – Heaviness and Tenderness 6. Vaginal Discharge – Cervix -erosion, dysplasia causes leucorrhoea 7. Chloasma 8. Weight Gain 9. Psychosexual Trouble – Depression, Loss of Libido 10. Others - Leg Cramps, Dimness of Vision
  • 39. MAJOR SIDE EFFECTS… • Cardiovascular Diseases 1) MI – Increased Risk in heavy smokers 2) Ischaemic Stroke - 1.5 times more 3) Haemorrhagic Stroke – double risk 4) Venous Thromboembolism – Risk increases with age, recent surgery and thrombophilia • Hypertension - In women more than 35 Yrs. • Carcinogenecity 1) Breast Cancer 2) Cervical Cancer
  • 40. INTERACTION WITH DRUGS… Contraception failure Increase COC activity Clearance decreased Carbamazepine Acetaminophen Amitriptyline Griseofulvin Erythromycin Caffeine Oxcarbazepine Fluoxetine Cyclosporine Phenobarbitol Fluconazole Diazepam Phenytoin Fluvoxamine Imipramine Primidone Grapefruit juice Phenytoin Rifampin Nefazadone Selegiline Ritonavir Vitamin C Theophylline St. John’s Wort Topiramate
  • 41. ABSOLUTE CONTRAINDICATIONS… (WHO CATEGORY IV) 1. Migraine, with focal Neurological Symptoms 2. Pregnancy and breast feeding ( 6 Months) 3. Severe Hypertension 4. Complicated valvular heart disease 5. D.M. with vascular complications 6. Active hepatitis, liver tumors 7. Major Surgery 8. Prolonged Immobilization .
  • 43. PROGESTIN ONLY CONTRACEPTIVES Oral pill 1973 Injectable suspension Intramuscular 1968 (1992 U.S.) Subcutaneous 2005 Subdermal Implant 6 LNG 1990 2 LNG 1996 1 ENG 2001 (2006 U.S) Intrauterine System (LNG) 2002
  • 44. MINI PILLS PREPARATIONS INDICATIONS : Age > 40 Yrs. Lactating Women. Norethindrone 0.350 mg Micronor/noriday Levonorgesterol 0.075 mg Neogest Norgesterol 0.030 mg Microval/norgeston Ethynodiol diacetate 0.500 mg Femulen Desogesterol 0.075 mg Cerazette/zerogen
  • 45. MECHANISM OF ACTION • Ovulation inhibition by decreased GnRH pulse frequency. • Suppression of midcycle LH and FSH surge • Thickened and decreased cervical mucus • Endometrial changes (atrophic endometrium)
  • 46. MINI PILLS Schedule • 1st day of M.C. and a backup method for 7 days • 6 wks after delivery – no backup method • Missed Tablet – Backup method for 48 Hrs. • Failure Rate - 3- 10 % Lactating Women – 0.5 % Advantages Can be used above 16 yrs of age, Smokers & obesity Best in DM, CVS Diseases & SLE Disadvantages Irregular Bleeding, Acne, Mastalgia, Amenorrhoea
  • 48. 1) Progesterone DMPA – 150 mg Depoprovera IM - Repeat every 3 Months NET-EN – 200 mg Norethisterone enanthate - Repeat every 2 months 2) Combined Cyclofem – DMPA 25 + Oestradiol cypionate 5 mg Mesigna - NET-EN 50 + Oestradiol Valerate 5 mg INJECTABLE CONTRACEPTIVES
  • 49. • Dose Schedule 5 to 7 days of menstruation Post- abortal – Immediate Post- delivery – 6 Wks • Technique : DMPA IM in arms NET-EN in buttocks ( Needs warming ) INJECTABLE CONTRACEPTIVES
  • 50. DEPO-SUBQ PROVERA 104  New formulation for subQ injection  30% lower dose (104 mg vs. 150 mg)  Rapid onset of action  Same effectiveness, same length of protection (>3 months)  Approved by USFDA (2005) and UK  Potential for home- and self-injection  Available for roll-out in 2011; Acceptability studies to begin in mid-2010 Uniject: • Single dose, single package • Prefilled, sterile, non-reusable • Short needles for subQ injection (easier use by non-clinical personnel/CHWs) • Compact; easy to use and store
  • 51. Mode of Action • Inhibits ovulation • Cervical mucus thickening • Endometrial alteration Eligibility criteria Adolescents > 16 yrs of Age Nulliparous Obese / Thin Smokers 6 Wks post delivery Post Abortal INJECTABLE CONTRACEPTIVES
  • 52. CONTRAINDICATIONS Absolute Pregnancy Unexplained genital bleeding Severe coagulation disorders Previous sex steroid induced liver adenoma Relative Liver disease Severe cardiovascular disease Severe depression Difficulty with injections
  • 53. Advantages • Easy & Convinient to use • Safe, no serious health effects • Free from estrogen related problems • Reduces menstrual flow & prevents anemia • Suitable for lactating women • Reduces risk- PID & vaginal candidiasis • Protects against endometrial cancer for 8 years after discontinuation Disadvantages • Irregular menstrual bleeding • Weight gain • Impaired glucose tolerance • Affection of fertility- delay • Risk of carcimona insitu & invasive cervical carcinoma in HIV • Bone density changes • Headache, weight gain, dizziness, abdominal pain, anxiety
  • 54. HORMONE RELEASING IUD  Progestasert  Levonorgestrel IUD 20 – LNG 20  T Shaped  Hormonal capsules in the vertical rod.  Maintains high local level of progesterone and low estrogen
  • 55. Progesterone IUD 38 mg of progesterone 65 mcg of Progesterone / Day Reduces Menstrual loss Disadvantage Costly 1 Yr. Life Insertion may require LA / Sedation HORMONE RELEASING IUD
  • 56. MIRENA 40 – 60 mg of LNG on stem. Release 20 mcg / Day Life 5 Years Failure Rate 0.1 to 0.4 % Difficult Insertion due to greater thickness Advantages – Contraception DUB
  • 57. IMPLANTS • Sub dermal drug delivery system • ADV: - long acting , reversible, progesterone only • TYPES OF IMPLANTS 1. Norplant – has 6 rods 2. Jadella & Norplant 2 – has 2 rods 3. Implanon – has 1 rod UNIPLANT • Single rod implant • Nomegestrol 38 mg. • Releases 100 microgm / day. • For 1 year.
  • 58. NORPLANT • 6 Silastic rod – 3.4 mm x 2.4 mm • 36 mg LNG • Daily release 50 – 80 mcg for 1st yr. 30 – 35 mcg over next 5 yrs. • Life 5 Yrs. • Insertion – Day 1 – 7 of M.C. Immediately after abortion 6 Wks after delivery
  • 59. TECHNIQUE  Arm / Forearm under the skin  Under L.A  Small incision made  6 rods inserted in fan shaped manner  Special trocar used for insertion  Effective within 24 Hrs.  Removal after 5 Yrs. under LA
  • 60. Mechanism • Suppression of Hypothalamic and pituitary hormones and prevents ovulation • Depresses endometrial growth • Cervical Mucus thickening Eligibility - Women of all ages Women who do not want pregnancy for several years Disadvantages 1) Trained person required for insertion and removal 2) Irregular bleeding 3) Infection 4) Hematoma 5) Removal may be difficult NORPLANT
  • 61. JADELLE / NOR PLANT II • 2 Solid Silastic rod • 44 mm x 2 mm • Inserted on medial aspect of upper arm • 70 mg of LNG – Release 30 to 35 mcg daily • Life 5 Years Norplant First month- 85µg 1year- 35µg 2year- 30µg Jadelle First month- 100µg 1year- 40µg 2year- 30µg
  • 62. IMPLANON • Long acting single rod subdermal implant • Length – 4 cm ,2mm diameter • DOSAGE: 68mg of crystalline etonorgestrel in ethylene vinyl acetate copolymer • DURATION : 3 years
  • 63. ADVANTAGES :  Long acting sustainable contraceptive  Low systemic side effects  Can be used by lactating mothers DISADVANTAGES :  Ectopic pregnancy- 1.3%  Local infection  EXPENSIVE  Has to insert & remove the capsules IMPLANON
  • 64. BIODEGRADABLE • Cipronor ( Single Capsule) – IMPLANTS : - LNG 26 mg - begins to disappear after 12 months. • INJECTABLE : - Microsphere of 0.06 – 0.1 mm diameter with Norethindrone with or without EE. - Given over Gluteal muscle. - Once injected , can’t be removed.
  • 65. How they work : • Hormones diffuse continuously from a reservoir within the ring into the bloodstream absorbed through vaginal epithelium • Combined vaginal rings prevents ovulation, thicken the cervical mucous & suppress the endometrial growth Side effects : leucorrhoea, vaginal discomfort, vaginitis, foreign body sensation, coital problems, expulsion CONTRACEPTIVE VAGINAL RINGS
  • 66. Combined progestin & estrogen rings Nestorone ring (Nestorone 150-200mcg + EE 15-20mcg/day) Effective 12 months (Phase III Trial) Emergency contraception Nuva ring (Etonogetrel 120mcg + EE 15mcg/day) Use for 3week & 1 ring-free week CONTRACEPTIVE VAGINAL RINGS
  • 67. Progesterone only rings (Progering) Less effective Preferred in lactating Progesterone 10mg/day - Effective up to 4 months Nestorone releasing ring - Effective up to 1 year Ulipristal in vaginal ring – Trial on going CONTRACEPTIVE VAGINAL RINGS
  • 68. • Nuva ring releases 15µg ethinyl estradiol & 120µg etonogestrel/day • Circulating hormones reach target within 24hrs & remains stable for 24hrs • Requires insertion of new ring every 4weeks • If ring is removed & not replaced within 3hrs-backup contraception for 7days reqiured. NUVA RING Failure rate 0.3%
  • 69. TRANSDERMAL CONTRACEPTION How they work • Patches release estrogen & progestin through the skin, prevents ovulation, thickening the cervical mucus, suppressing endometrial growth • User replaces patch weekly for 3 weeks & 1 patch free week 3 layers : a. Outer - polyester protective layer b. Middle - medicated adhesive layer c. Inner - polyester release liner  Ortho Evra  (EE 20mcg + Norelgestromin 150mcg / day)  Gestadone patch  (EE 18mcg + Gestadone 50mcg/ day)
  • 70. TRANSDERMAL CONTRACEPTION Spray on contraceptive (Nestorone) Single daily progestin only spray-on* Absorbed into the skin & diffuses into the blood stream Inhibits ovulation The Metered Dose Transdermal System - spray* (*Phase 1 trial …..Australia ) Gel (Nestrone) Single daily application
  • 71. CENTCHROMAN ( SAHELI ) • Ormeloxifene . • research product of CDRI , Lucknow • Non steroidal , potent anti estrogenic , weak estrogenic. • Prevent implantation of fertilized ovum . • Orally 30 mg twice weekly for first 3 months then once a week. • Avoided in PCOD, liver , kidney disease.
  • 73. MALE HORMONAL METHODS New male pill • Desogestrel + Testosterone • Blocks the production of sperm - maintaining male characteristics & libido • Daily pill • 100% effective and completely reversible in preliminary clinical trials • In clinical trials, all of the participants’ sperm counts dropped to zero, which means that the male pill would be more effective than the condom and even the female pill.
  • 74. CatSper blocker • Sperm rely on calcium ions in sperm tail for mobility & fertilization • Humans -ion-channel gene - CatSper. • Blocking CatSper action - effective form of birth control • Men or women could take this potential CatSper “blocker” • It acts ”wherever sperm are present” • Active only in fully developed sperm MALE HORMONAL METHODS
  • 75. GENDARUSSA • First non hormonal male contraceptive pills. • Developed by Indonesia. • Active ingredient in Gendarussa disrupts an enzyme in the sperm head, which weakens the ability of the sperm to penetrate the ovum. • The effect is short term and reversible – having no effect on male hormones. • Still under clinical trials…
  • 76. The Male Patch (Adjudin) Adjudin (2,4-dichlorobenzyl- 1H-indazole-3-carbohydrazide) Non-hormonal male contraceptive Acts by blocking maturation of sperm in the testes No effect on testosterone production • Normal spermatogenesis returned in 95% within 210 days after the drug had been discontinued • The oral dose effective for contraception - high : causing side effects in muscles & liver Patch or implant – Avoids 1st pass metabolism MALE TRANSDERMAL PATCH
  • 77. REFERENCES • S Rowlands. New technologies in contraception. BJOG 2009; 116:230-239. • Allen RH, Goldberg AB, Grimes DA. Expanding access to intrauterine contraception. American Journal of Obstetrics and Gynecology 2009;201(5):456-61. • Grimes DA, Lopez LM, Schulz KF, Immediate post-partum insertion of intrauterine devices Review, published in The Cochrane Library2010, Issue 5. • WHO, Family Planning A GLOBAL HANDBOOK FOR PROVIDERS Update 2011. • “Guidelines for administration of emergency contraceptive pills by medical officers,” Research Studies and Standard Division, Department of Family Welfare, Government of India, June 2009. • The essentials of Contraceptive Technology, a handbook for clinic staff, John Hopkins Population Information Program, 2010.