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
Kapvay details?
clonidine
• BID (maintenance)
• 0.1 mg and 0.2 mg ER tablet
• Indicated for ADHD
Fentanyl Trades?
Duragesic, Actiq, Onsolis, Fentora, Abstral, Lazanda
Duragesic details
fentanyl • q72h • 12.5, 25, 50, 75, 100 mcg/hr • ***Reservoir system • Indicated for chronic pain (12 hour onset) • Contains alcohol USP • Fold over on itself to discard
Actiq details
fentanyl • q4h • Transmucosal lozenge on a stick • Rub on side of cheek for 15 minutes • Hold under hot water to dissolve
Onsolis details?
fentanyl • q2h • Transmucosal buccal film • Applied to the inside of the cheek • Flush down toilet to discard
Fentora details?
fentanyl
• q4h
• Buccal tablet
• Flush down toilet to discard
Abstral details?
fentanyl
• q2h
• Sublingual tablet
• Flush down toilet to discard
Lazanda details?
fentanyl • q2h • Nasal spray • 1 spray in 1 nostril • Spray extra into provided pouch → place in child resistant container → discard
First transdermal system?
scopolamine
scopolamine indications?
prevention of nausea and vomiting
2 directions for scopolamine?
- Motion sickness: place behind ear 4 hours before needed; may leave on 3 days
- Surgery: apply patch the evening before surgery
directions for after application of scopolamine?
- Wash hands thoroughly after applying or removing because it may cause mydriasis
- Most common side effect is dry mouth and drowsiness
scopolamine Trade and details?
Transderm-Scop
• 5 mcg/hr
• Anticholinergic agent
• Adhesive matrix
lidocaine Trade?
Lidoderm
Lidoderm details?
lidocaine • qday -5% • Adhesive matrix without a P.A.E. • Local anesthetic • Indicated for pain associated PHN • Apply up to 3 patches/day at the same time; put one on for 12 hours, then remove for 12 hours
gabapentin Trade?
Neurontin
Neurontin generic and details?
gabapentin
• Indicated for PHN and partial seizures
pregabalin Trade?
Lyrica
Lyrica generic and details?
pregabalin
• Indicated for PHN, partial seizures, DPN, and fibromyalgia
Chicken pox vaccine?
Varivax - varicella vaccine
for children and adults
shingles vaccine?
Zostavax - zoster vaccine
prevents reactivation of the varicella virus, must be 50+ years old
Anticholinergic indication, symptoms, and side effects:
can be used for overactive bladder
• Symptoms: urinary incontinence, urgency, and frequency
• Side effects: xerostomia, constipation, sedation, mydriasis, and hyperthermia
Trades of oxybutynin?
Oxytrol, Ditropan, Ditropan XL, Gelnique
anticholinergics
Oxytrol details?
oxybutynin (anticholinergic)
• Twice weekly
• 3.9 mg/24 hours transdermal
• Adhesive matrix
Ditropan details?
oxybutynin (anticholinergic)
IR tablet
ER tablet - Ditropan XL
Gelnique details?
oxybutynin (anticholinergic)
• qday
• 10% topical gel
• Individually wrapped packets of gel → applied to abdomen
• Contains percutaneous absorption enhancer
tolterodine Trade?
Detrol, Detrol LA
anticholinergic
Detrol generic?
tolterodine IR - tablet
Detrol LA - tolteridone ER - CAPSULE
anticholinergic
trospium Trade?
Sanctura, Sanctura XR
anticholinergic
Sanctura generic and details?
trospium IR tablet - empty stomach
Sanctura XR - tropsium ER capsule - empty stomach
anticholinergic
darifenacin Trade?
Enablex
anticholinergic
Enablex generic?
darifenacin
anticholinergic
solifenacin Trade?
Vesicare
anticholinergic
Vesicare generic?
solifenacin
anticholinergic
Toviaz generic?
fesoterodine
anticholinergic
fesoterodine Trade?
Toviaz
anticholinergic
mirabegron Trade?
Myrbetriq
Myrbetriq generic and details?
mirabegron
• relaxes bladder smooth muscle
• Beta-3 agonist
• NOT anticholinergic
methylphenidate Trade?
Daytrana
Daytrana generic and details?
methylphenidate • qday • 10, 15, 20, 30 mg/9 hours • Adhesive matrix • Indicated for ADHD • Wear on hip 2 hours before needed, then take off 9 hours later • CII
selegiline Trades?
Emsam, Eldepryl, Zelapar
Emsam generic and details?
selegiline • qday • 6, 9, 12 mg/24 hours • Adhesive matrix • MAOI antidepressant • Indicated for depression • Be careful with tyramine if taking 9 mg or 12 mg; avoid pseudoephedrine and phenylephrine
Eldepryl generic and details?
selegiline (MAOI)
• Capsule
• Antiparkinson’s agent
Zelapar generic and details?
selegiline (MAOI)
• ODT
• Antiparkinson’s agent
granisetron Trade?
Sancuso
antiemetic
Sancuso generic and details?
granisetron
• qweek
• 3.1 mg/24 hours - Adhesive matrix
• Antiemetic - Indicated for N/V patients receiving chemotherapy for 5 straight days; works in the CTZ
• Apply on upper arm 24 hours before first treatment → take off 24 hours after last treatment
• May cause phototoxic reaction:avoid sun exposure for 10 days after removal
Aloxi generic?
palonosetron
antiemetic
palonosetron Trade?
Aloxi
antiemetic
Anzemet generic?
dolasetron
antiemetic
dolasetron Trade?
Anzemet
antiemetic
Zofran generic?
ondansetron
ondansetron Trade?
Zofran
Emend generic?
aprepitant
antiemetic
aprepitant Trade?
Emend
antiemetic
Cholinesterase Inhibitors indication?
Alzheimer’s Disease
inhibit cholinesterase → increase ACh levels in the brain
o Side effect: N/V if dose is too high
rivastigmine Trade?
Exelon Patch
cholinesterase inhibitor
Exelon generic and details?
rivastigmine • qday • 4.6, 9.5 mg/24 hours • Adhesive matrix • 4.6 mg x 1 month, then increase to 9.5 mg as maintenance dose • Apply patch in the middle of the back
Aricept generic?
donepezil
cholinesterase inhibitor
Razadyne generic?
galantamine
cholinesterase inhibitor
donepezil Trade?
Aricept
cholinesterase inhibitor
galantamine Trade?
Razadyne
cholinesterase inhibitor
buprenorphine Trades?
Butrans and Buprenex
+ non-trade sublingual tab
Butrans details?
buprenorphine
• qweek
• 5, 10, 20 mcg/hour
• Adhesive matrix
• Opioid analgesic
• Once patch is removed do not use the same skin for 3 weeks
• 10 and 20 mcg/hour are used in opioid intolerant patients
Buprenex details?
parenteral buprenorphine
opioid analgesic
oral buprenorphine
opiod analgesic
• Sublingual tablet
• Indicated for addiction
diclofenac epolamine Trade?
Flector Patch
Flector generic and details?
diclofenac epolamine (patch) • BID • 1.3% adhesive matrix • NSAID → inhibits cyclooxygenase-2 • Indicated for strains (stretched muscle) and sprains (stretched ligament) • Do not use if allergic to aspirin
smoking cessation generics?
buproprion, varenicline, nicotine
buproprion Trade?
Zyban
smoking cessation
Zyban generic and details?
buproprion
• 150 mg tablet
• Take 1 tablet x 3 days, then BID x 12 weeks
• Aminoketone antidepressant
• Indicated only for smoking cessation
• Start 1 week before trying to quit to give drug a chance to reach therapeutic levels
• Rx only
varenicline Trade?
Chantix
smoking cessation
Chantix generic and details?
strength, dosing, class, MOA, side effects, BBW
varenicline
• 0.5 mg and 1 mg tablet
• Take 0.5 mg qday x 3 days, then 0.5 mg BID x 4 days, then 1 mg BID x 12 weeks
• Nicotine receptor agonist
• Varenicline binds to its receptor and produces nicotine-like effects and inhibits nicotine
• Side effects: N/V (take with food to help), vivid dreams, violent behavior
• BBW: 1. may cause neuropsychiatric events. 2. Do not use in patients with depression, BD, or schizophrenia
• Rx only
nicotine Trades?
Nicorette, Nicorette DS, Nicotrol Inhaler, Nicoderm CQ, + no-trade lozenges
Nicorette dosing details?
nicotine
• 2 mg nicotine gum; 30 maximum pieces a day
• DS: 4 mg nicotine gum; 20 maximum pieces a day
• Patients smoking >25 cigarettes a day should start with 4 mg
Nicorette delivery details?
- Contains a sugar free base to allow systemic delivery; absorbed via buccal mucosa in alkaline saliva → avoid swallowing and beverages that make saliva acidic
- Tempted to smoke → chew 1 piece until peppery taste/tingling is perceived → place between cheek and gum until taste is gone → repeat for ~30 minutes
nicotine lozenges details?
- 2 mg and 4 mg nicotine lozenge (OTC)
- Dose depends on “time to first cigarette”; needs alkaline saliva
- 4 mg: within 30 minutes of waking up
- 2 mg: after 30 minutes of waking up
- Take 1 lozenge q1-2h x 6 weeks, then q2-4h x 3 weeks, then q4-8h x 3 weeks
Nicotrol details?
nicotine inhaler
• 4 mg cartridge; max dose/day = 16 cartridges
• Contains enough nicotine for 20 minutes of active puffing
• Transmucosal so do not inhale into lungs
• Rx only
Nicoderm strengths and application instructions?
- qday
- 7 mg, 14 mg, 21 mg/hr adhesive matrix
- Apply to area on upper part of arm → remove after 24 hours (do not reuse this site for 7 days) and apply new patch to different site → fold patch in half to discard
Nicoderm dosing instructions?
- Dosing is based on how many cigarettes/day smoked
- > 10 cigarettes: 21 mg – 6 weeks, 14 mg and 7 mg– 2 weeks
- <10 cigarettes: 14 mg – 6 weeks, 7 mg – 2 weeks