Transdermal Drug Delivery Systems Flashcards
2 types of transdermals
- adhesive matrix
- reservoir
2 advantages of transdermals
- avoid 1st pass effect by the liver
- increase pt. compliance
adhesive matrix
- drug is evenly distributed, so can be cut in half
- contains a release liner and drug is released from adhesive
reservoir
- cannot be cut because drug would leak
- contains a rate-controlling membrane and a reservoir filled with drug formulation
- adhesive on both sides, not in the middle
flux
rate of diffusion through the skin
Minitran, Nitro-Dur
nitroglycerin transdermal system
- category: vasodilator
- ind. for prevention of angina pectoris
- adhesive matrices
- Minitran: 0.1mg/hr
- main side effect: headache (usually diminishes over time)
how to minimize nitroglycerin tolerance?
wear for 12 hours and remove for 12 hours
Ranexa
ranolazine
- category: vasodilator
- ind. for prevention of angina
- BID
- tab: 500mg, 1000mg
estradiol
an estrogen hormone ind. for hormone replacement therapy (HRT) in post-menopausal women
BBW: increase risk of CVD and dementia in post-menopausal women, increase risk of endometrial cancer in pre-menopausal women
Climara
estradiol adhesive matrix system
- ind. for VM, VA, and O
- qweek
- strengths: 0.025mg/24hr, 0.0375, 0.05, 0.06, 0.075, 0.1
atrophic vaginitis
inflammation of the vagina due to thinning and shrinking of tissues, caused by decreased estrogen levels
-estradiol restores normal vaginal mucosa
symptoms of vaginal atrophy
soreness, pain during intercourse, bleeding during intercourse
dyspareunia
painful intercourse
Vivelle-Dot
estradiol adhesive matrix system
- ind. for VMS, VA, O
- BIW
- strengths: 0.025mg/24hr, 0.0375, 0.05, 0.075, 0.1
Alora
estradiol adhesive matrix system
- ind. for VMS, VA, O
- strengths: 0.025mg/24hr, 0.05, 0.075, 0.1
Menostar
estradiol adhesive matrix system
- ind. ONLY for O
- low dose estrogen
- qweek
- one strength: 0.014mg/24hr
Estrasorb
estradiol topical emulsion (0.05mg/2 packets)
- ind. for VMS, VA, O
- individually wrapped packets of estradiol
- qAM
- -one packet on left leg and right leg for 3 minutes
- -rub excess on buttocks
- contains soybean oil and alcohol USP
Evamist
estradiol transdermal spray 0.021mg/spray
- ind. for VMS, VA, O
- qday
- spray on inside of forearm
- contains alcohol USP and octisalate
Divigel
estradiol topical gel 0.1% (30 packets/box)
- ind. for VMS, VA, O
- qday - apply one packet to upper thigh
- individually wrapped packets of gel:
- -0.25g(0.25mg of estradiol), 0.5g(0.50mg), 1g(1mg)
- contains alcohol USP
Femring
estradiol vaginal ring
- ind. for VMS, VA, O
- strengths: 0.05mg/24hr, 0.1mg
- can be felt during sex, can come out during sex or when straining with a bowel movement
- -if it comes out, wash off and reinsert
Vagifem
estradiol vaginal tablet (10mcg)
- ind. for VA
- tablet inserted with applicator
- initial: 1 qday x 2 weeks, then 1 tab BIW
Premarin Vaginal Cream
conjugated/equine estrogens vaginal cream
- ind. for VA
- BIW
- 0.625mg/g cream
- applicator calibrated in 0.5g increments up to 2g
- derived from the urine of pregnant horses
Climara Pro
estradiol, levonorgestrel adhesive matrix system
- ind. for VMS, O
- qweek
progestin
synthetic progesterone
CombiPatch
estradiol, norethindrone adhesive matrix system
- ind. for VMS, VA
- BIW
- refrigerate in the pharmacy, pt. can store at RT
levonorgestrel, norethindrone, norelgestromin
progestins
Activella
estradiol, norethindrone
- ind. for VMS, VA, O
- qday
- oral tablet: 0.5mg estradiol/0.1mg norethindrone, 1mg/0.5mg
Ortho Evra
ethinyl estradiol, norelgestromin adhesive matrix system
- ind. for contraception
- apply 1 patch every week for 3 weeks, 1 week off, then repeat
Androderm
testosterone reservoir patch system
- ind. for male hypogonadism
- strengths: 2mg/24hr, 4mg/24hr
- contains alcohol USP
- don’t use the same site more than once per week because it causes irritation
anabolic steroids
- synthetic derivatives of testosterone
- may cause hepatotoxicity and paranoid jealousy
men’s normal daily production of testosterone
5mg/day
Anabolic Steroids Control Act
made all anabolic steroids schedule 3 drugs
hypogonadism
decreased activity of the gonads so insufficient secretion of testosterone
-decreased libido and energy
libido
sex drive
AndroGel
testosterone topical gel
- qday
- absorb 10% of dose
- single dose packets: 2.5g(25mg), 5g(50mg)
- -rub contents of 1 packet on shoulder
- metered-dose pump: 1%(1 pump contains 12.5mg) X4= 50mg, 1.62%(1 pump contains 20mg) X2=40mg
- apply to shoulders or arms
Testim
testosterone single dose packets
- qday
- 5g(50mg)
Fortesta
testosterone metered-dose pump
- qday
- 1 pump contains 10mg X4 pumps= 40mg
- 2 pumps are applied to each thigh which minimizes secondary exposure
Axiron
testosterone
- qday
- topical solution
- metered-dose pump: 1 pump contains 30mg X 2(1 under each arm) = 60mg
- -spray 1 pump in cup and apply under each arm like roll-on deodorant
BBW for testosterone
secondary exposure in women and children can cause virilization
-wash hands after use and avoid women and children
virilization
development of masculine characteristics