TRANSDERMAL HORMONAL CONTRACEPTION Prof. Aboubakr Elnashar

1. TRANSDERMAL HORMONAL
CONTRACEPTION
Prof. Aboubakr Elnashar
Benha University Hospital, Egypt
Email: elnashar53@hotmail.com
Aboubakr Elnashar

2. Missed pills
50% of pill users missed 3 pills/pack by the 3rd cycle of
oral contraceptive use
(Potter et al.,2001)
Aboubakr Elnashar

3. Contents
•Advantages
•Formulations
Description of the Patch
Instruction for use
Patch adhesion
Pharmakokinetics
Side effects
Contraindication
Patient satisfaction
Compliance
Efficacy
Conclusion
Aboubakr Elnashar

4. Advantages
(Burkman, 2007)
Continuous, sustained release:
avoids peak& low drug levels
Longer dosing interval:
improves patient compliance
Avoids first-pass:
met& enzymatic degradation by GIT
induction of hepatic protein synthesis e.g. extrinsic clotting
factors.
Aboubakr Elnashar

5. TD:
Can be given when oral route is not suitable
Unaffected by vomiting or diarrhea.
Drug administration stops with patch removal
Aboubakr Elnashar

6. Formulations
ORTHO EVRA: FDA 2001
0.75 mg EE
6.0 mg norelgestromin: active metabolite of
norgestimate:
(Cilest: EE, 30ug, Norgestimate, 250 Ug)
Aboubakr Elnashar

7. EVRA
0.6 mg EE
6.0 mg Norelgestromin
Daily delivery
rate
150 ugNGMN
20 ugEE
Aboubakr Elnashar

8. Mode of action
•Suppress
ovulation similar to OCs.
follicular development.
•Reduce cervical mucus scores, more hostile to
sperm penetration.
•Induce progestational endometrium and reduce
endometrial thickness.
Aboubakr Elnashar

9. Description of the Patch
3 separate layers:
 Lower: packing, light brown,
flexible 4.5 x 4.5 cm
 Middle: adhesive, contains the
active hormones
 Top: protecting the adhesive layer
& removed prior to application
Aboubakr Elnashar

10. Instruction for use
4 sites:
Upper Torso
(excluding the breasts)
Upper outer arm
Lower abdomen
Buttock
Two consecutive patches should not be placed over
the exact same area.
Hormonal absorption from the lower abdomen is 20%
lower than that from the other 3 sites
Aboubakr Elnashar

11. Regimen:
• One patch/w for 3ws, followed by a patch-free w.
• The first patch should be placed on 1st day of the
menstrual cycle
• If a patch change is missed for 2 d:
clinical efficacy is maintained: backup contraception
is not needed.
Aboubakr Elnashar

12. When initiating:
• After childbirth and no-breast feeding:
Wait 4 w
Backup contraception for 7 days.
• After a first-trimester miscarriage:
immediately (the same day).
Backup contraception is not necessary if the patch is
started within 5 days.
Aboubakr Elnashar

13. Patch adhesion
Patch to the abdomen
(Zacur et al, 2002)
Showers, sunbathing, strenuous exercise, sauna,
whirlpool, treadmill, swimming:
Adhesive reliability was maintained for 7 d
1.8%: replaced {fell off}
2.9%: replaced {partial detachment }
Aboubakr Elnashar

14. Pharmakokinetics
ORTHO EVRA patch Vs OCs (FDA)
1. Higher EE steady concentrations:
AUC & average concentration at steady state for EE
are 60% higher
2. lower EE peak concentrations.
25%
Increased estrogen exposure: increase the risk of
adverse events, including VTE.
Aboubakr Elnashar

15. Aboubakr Elnashar

16. 3. Coagulation factors
(antithrombin III, tProtS and fProtS):
No significant differences
(Johnson et al, 2006).
Higher EE levels seen with the patch
might not have any greater hepatic impact than lower
EE levels seen with the pill.
Aboubakr Elnashar

17. Side effects
1. VTE
Jick et al, 2006, 2007, 2010
Risk is similar to that for users of OCs
Cole et al, 2007:
increased risk of with the patch Vs OCs
VTE /100,000 women years:
Patch: 40.8
OCs: 18.3
Aboubakr Elnashar

18. little or no increasedVTE
Contraindicated: in high risk forVTE:
Safe
Aboubakr Elnashar

19. 2. Headache& nausea:
The most frequent adverse events
(Sibai et al, 2002)
Aboubakr Elnashar

20. 3. Breast symptoms:
(discomfort, engorgement, pain)
more with patch than OCs during cycles 1& 2 only
with continued use, decreased to none during cycle
13
(Sibai et al, 2002)
Aboubakr Elnashar

21. 4. Dysmenorrhea
greater in patch than in OC users
(13.3% Vs 9.6%)
(Sibai et al, 2002)
5. BTB:
Low& similar to those with OCs
(Zieman et al, 2002).
Aboubakr Elnashar

22. 6. Application site reactions
Mild or moderate
20%
Discontinuation: 2.6%
(Sibai et al, 2002)
Aboubakr Elnashar

23. 7. Changes in wt.
Minimal
Use for 13 cycles:
2.2%: wt gain of 10%
1.4%: wt loss of 10%.
Comparable to OCs
(Sibai et al, 2002)
With the exception of application site reactions,
patch is well tolerated
adverse events are similar to that of OCs.
Aboubakr Elnashar

24. Aboubakr Elnashar

25. Contraindications
• Identical to those for OCs
• Exceptions.
1. Active skin conditions: which could alter the rate
of hormonal absorption
2. Dermatologic conditions that would be worsened
by patch application.
• On the other hand
patches are used when pills can not be used e.g. GIT
absorption problems
Aboubakr Elnashar

26. Patient satisfaction
Emotional
Physical well-being
Improvements in premenstrual symptoms
Higher than OCs
(Urdl et al, 2005).
: Significantly better compliance: fewer unintended
pregnancies
European multinational study (2011)
High levels of women's satisfaction and
compliance with TD contraception
Aboubakr Elnashar

27. Compliance
Consistent & correct use
(89% Vs. 79%).
Compliance was higher for the patch
(Cochrane systematic review, Gallo et al, 2003; Audet et al, 2001)
Aboubakr Elnashar

28. Efficacy
Overall& method failure:
Method failure: 0.4 %
User failure: 0.1%
Efficacy:
Higher {higher rates of correct& consistent use of
patch}
Similar
(Cochrane systematic review, Gallo et al, 2003)
less effective
Wt >90 kg
(Zieman et al, 2002)
Aboubakr Elnashar

29. Conclusion
TD C patch compared to COs:
Similar efficacy& adverse effects
 Higher satisfaction & compliance
 Easier to use
 More suitable for today’s active lifestyles
Aboubakr Elnashar

30. Benha University Hospital, Egypt
Email: elnashar53@hotmail.com
Prof. Aboubakr Elnashar
Aboubakr Elnashar