Transdermals and related drugs Flashcards
rate of diffusion through the skin?
Flux
Adhesive matrix?
drug is evenly distributed, can be cut in half, contains a release liner, and drug is released from the adhesive
Reservoir matrix?
cannot be cut in half because the drug would leak, adhesive on both sides, has a rate controlling membrane, and reservoir filled with drug formulation
Nitroglycerin indications:
vasodilators indicated for prevention of angina pectoris
will not relieve acute attack
Nitroglycerin side effects:
headache due to vasodilation
2 nitroglycerin Trades?
Minitran and Nitro-Dur
Minitran details?
nitroglycerin • 0.1 mg/hr • qday • Adhesive matrix • Minimize tolerance by wearing for 12 hours → remove for 12 hours
Nitro-Dur details?
nitroglycerin
• qday
• Adhesive matrix
• Minimize tolerance by wearing for 12 hours → remove for 12 hours
Ranexa generic?
ranolazine
ranolazine Trade and details?
Ranexa
vasodilator (not relieve acute attack)
• 500 and 1000 mg TABLET
• BID
Estrogen hormone for hormone replacement therapy?
estradiol
hot flash order of events?
• Loss of ovarian estrogen secretion after menopause → instability of thermoregulation → hot flash
inflammation of the vagina due to thinning/shrinking of tissues
atrophic vaginitis
painful intercourse
dyspareunia
2 BBW for estradiol?
- BBW: increases risk of CVD and dementia in post-menopausal women
- BBW: increase risk of endometrial cancer in pre-menopausal women
estradiol indications?
• Indicated for vasomotor symptoms, vaginal atrophy, and osteoporosis (exception: Menostar)
5 Trades for estradiol transdermal products?
Climara, Vivelle-Dot, Alora, Minivelle, Menostar
Climara details?
estradiol
• qweek
• 0.025, 0.0375, 0.05, 0.06, 0.075, 0.1 mg/24 hours
• Adhesive matrix
Vivelle-Dot details?
estradiol
• twice weekly
• 0.025, 0.0375, 0.05, 0.06, 0.075, 0.1 mg/24 hours
• Adhesive matrix
Alora details?
estradiol
• twice weekly
• 0.025, 0.05, 0.075, 0.1 mg/24 hours
• Adhesive matrix
Minivelle details?
estradiol
• twice weekly
• 0.0375, 0.05, 0.075, 0.1 mg/24 hours
• Adhesive matrix
Menostar details?
estradiol • qweek • 0.014 mg/24 hours • Only indicated for osteoporosis • Adhesive matrix
estradiol (only) other products - 6
even eating dicks feels very eerie
Estrasorb, Evamist, Divigel, Femring, Vagifem, Estrace
Estrasorb details?
estradiol
• 2 packets qAM
• Topical emulsion
• 0.05 mg/2 packets: one packet each leg for 3 minutes, excess on buttocks
• Indicated for VM
• Alcohol USP is used as a P.A.E.
• Contains soybean oil; do not take if allergic to peanuts
Evamist details?
estradiol • 1 spray qday • 0.021 mg/spray transdermal spray • Indicated for VM • Spray on inside of arm • Alcohol USP and octisalate are the percutaneous absorption enhancers
Divigel details?
estradiol
• qday
• 0.1% topical gel: 0.25, 0.5, 1 g packets of gel
• Indicated for VM
• Apply one packet to upper thigh
• Alcohol USP is used as a percutaneous absorption enhancer
Femring details?
estradiol • q3months • Vaginal ring • 0.05 and 0.1 mg/24 hours • Indicated for VM and VA
Vagifem details?
estradiol • 10 mcg vaginal tablet • Indicated for VA • Initial: 1 tablet qday x 2 weeks • Maintenance: 1 tablet twice weekly
Estrace details?
estradiol • 0.1 mg/g vaginal cream • Indicated for VA • Initial: qday x 2 weeks → after 2 weeks use ½ dose qday x 2 weeks • Maintenance: 1-3x/week
conjugated equine estrogens Trade?
Premarin Vaginal Cream
Premarin Vaginal Cream generic and details?
conjugated equine estrogens
• BIW 0.625mg/g vaginal cream
• Indicated for VA
• derived from pregnant horse urine
Climara Pro generic and details?
estradiol, levonorgestrel
• Qweek
• Adhesive matrix
• Indicated for VM and O
estradiol, levonorgestrel Trade?
Climara Pro
estradiol norethindrone Trades?
CombiPatch and Activella
CombiPatch details?
estradiol, norethindrone • Twice weekly • Adhesive matrix • Indicated for VM and VA • Refrigerate in the pharmacy
Activella details?
estradiol, norethindrone • qday • 0.5 mg/0.1 mg tablet • 1 mg/0.5 mg tablet • Indicated for VM, VA, and O
Ortho Evra generic and details?
ethinyl estradiol, norelgestromin • qweek • Adhesive matrix • Indicated for contraception • Apply 1 patch qweek x 3 weeks → patch-free for 1 week → repeat
ethinyl estradiol, norelgestromin Trade?
Ortho Evra
Testosterone produced by men?
5mg/day
synthetic derivatives of testosterone?
anabolic steroids
anabolic steroid legislation?
Anabolic Steroids Control Act- makes all CIII drugs
decreased activity of the gonads → insufficient secretion of testosterone → no libido ?
male hypogonadism (Libido - sex drive)
testosterone drug BBW:
secondary exposure in women and children can cause virilization → wash hands after use
testosterone drug interactions:
testosterone decreases anticoagulant and insulin requirements
testosterone Trades? (5)
Adam always tries fornication annually
Androderm, AndroGel, Testim, Fortesta, Axiron
Androderm details?
testosterone • qday • 2 mg/24 hours and 4 mg/24 hours • *****Reservoir patch • Contains alcohol USP • Do not use the same site more than once per week → irritation
AndroGel details?
testosterone
• Qday
• Single dose packet: 2.5 g, 5 g = 25 mg, 50 mg testosterone → 2.5 mg, 5 mg absorbed via the shoulder
• Metered dose pump: 1% (1 pump=12.5 mg x 4 pumps) = 50 mg → 5 mg absorbed via the shoulder, 1.62% (1 pump=20 mg x 2 pumps) = 40 mg testosterone → 4 mg absorbed via the shoulder
Testim details?
testosterone
• qday
• 5 g single dose packets = 50 mg testosterone → 5 mg absorbed
Fortesta details?
testosterone
• qday
• Metered dose pump
• 2 pumps applied to each thigh to minimize secondary exposure
• 1 pump = 10 mg testosterone x 4 pumps = 40 mg → absorb 4 mg
Axiron details?
testosterone • qday • Topical solution • Metered dose pump: 1 pump = 30 mg testosterone x 2 pumps (1 under each arm) = 60 mg → 6 mg absorbed • Contains alcohol USP
clonidine Trades?
Catapres TTS and Kapvay
Catapres TTS details?
clonidine • qweek • 0.1, 0.2, 0.3 mg/24 hours • Reservoir system • Indicated for hypertension • Transdermal Therapeutic System • Optional adhesive overlay to keep patch on