transdermal hormonal contraception prof. aboubakr elnashar
DESCRIPTION
TRANSDERMAL HORMONAL CONTRACEPTION Prof. Aboubakr ElnasharTRANSCRIPT
TRANSDERMAL HORMONAL
CONTRACEPTION Prof. Aboubakr Elnashar
Benha University Hospital, Egypt Email: [email protected]
Aboubakr Elnashar
Missed pills 50% of pill users missed 3 pills/pack by the 3rd cycle of
oral contraceptive use (Potter et al.,2001)
Aboubakr Elnashar
Contents •Advantages
•Formulations
Description of the Patch
Instruction for use
Patch adhesion
Pharmakokinetics
Side effects
Contraindication
Patient satisfaction
Compliance
Efficacy
Conclusion
Aboubakr Elnashar
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
TD:
Can be given when oral route is not suitable
Unaffected by vomiting or diarrhea.
Drug administration stops with patch removal
Aboubakr Elnashar
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
EVRA 0.6 mg EE
6.0 mg Norelgestromin
Daily delivery
rate
150 ug
NGMN
20 ug
EE
Aboubakr Elnashar
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
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
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
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
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
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
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
Aboubakr Elnashar
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
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
little or no increased VTE Contraindicated: in high risk for VTE: Safe
Aboubakr Elnashar
2. Headache& nausea:
The most frequent adverse events (Sibai et al, 2002)
Aboubakr Elnashar
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
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
6. Application site reactions Mild or moderate
20%
Discontinuation: 2.6% (Sibai et al, 2002)
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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
Aboubakr Elnashar
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
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
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
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
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