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
testosterone drug interactions
decreases anticoagulant and insulin requirements
Catapress-TTS
clonidine reservoir system
- ind. for HTN
- 0.1mg/24hr, 0.2mg, 0.3mg
- contain optional adhesive overlay covers to keep patch on
- DON’T stop cold turkey, switch to tablets and then taper*
Kapvay
clonidine ER tablet
- ind. for ADHD
- strengths: 0.1mg, 0.2mg
- maintenance dose BID
Duragesic
fentanyl reservoir system (CII)
- ind. for chronic pain
- opioid-naive pts: 12.5mcg/hr, 25mcg/hr
- opioid-tolerant pts: 50, 75, and 100 mcg/hr
- commonly abused
- contains alcohol USP
Actiq
fentanyl lozenge on a stick
- opioid analgesic
- rub on inside of cheek for about 15 mins
- onset in approx. 15 mins
Onsolis
fentanyl buccal film
- opioid analgesic
- apply to inside of cheek
Fentora
fentanyl buccal tablet
-opioid analgesic
Abstral
fentanyl sublingual tablet
-opioid analgesic
Lazanda
fentanyl nasal spray
- opioid analgesic
- 1 spray in 1 nostril
Transderm-scop
scopolamine adhesive matrix system
- anticholinergic agent
- ind. for prevention of N/V assoc. with motion sickness and in pts. recovering from anesthesia after surgery
- motion sickness: place behind ear 4hr before needed, may leave on up to 3 days then put new patch behind other ear if needed
- surgery: apply 1 patch the evening before surgery
- pt. counseling: wash hands thoroughly after applying or removing b/c it may cause mydriasis and most common adverse effects are dry mouth and drowsiness
Zyban
bupropion
- aminoketone antidepressant
- ind. ONLY for smoking cessation
- start 1 week before trying to quit to give drug a chance to reach therapeutic levels
- tablet: 150mg, take 1 qday X 3D, then BID X 12 weeks
Wellbutrin
bupropion
- aminoketone antidepressant
- ind. ONLY for depression but will work for smoking cessation
Chantix
varenicline
- nicotine receptor agonist
- tablet: 0.5mg, 1mg
- side effects: N/V(take with food), vivid bad/weird dreams, violent behavior(#1 drug that causes this)
- BBW: do not use in pts. with depression, bipolar disorder, or schizophrenia*
Minivelle
estradiol transdermal system
- ind. for VMS, VA, O
- BIW
Nicorette Gum
nicotine (OTC)
- ind. as an aid to smoking cessation for the relief of nicotine withdrawal symptoms
- contains a sugar free base that provides systemic delivery of nicotine - will not work if swallowed
Nicorette
nicotine 2mg (OTC) -pts. who smoke 25 or less cigarettes per day start with this strength
Nicorette DS
nicotine 4mg (OTC) -pts. who smoke >25 cigarettes per day should start with this strength
Nicorette pt. counseling
- absorbed through the buccal mucosa, avoid swallowing as much as possible
- rate and extent of nicotine absorption is pH dependent (needs alkaline saliva), so avoid coffee, soft drinks, fruit juices, etc. that make saliva acidic
- do not chew continuously - when tempted to smoke, chew 1 piece until the peppery taste or tingling is perceived then place between cheek and gum until taste is gone, repeat in about 30 mins.
nicotine lozenge
- OTC
- 2mg, 4mg dep. on time to first cigarette
- -after 30 min. of waking is 2mg
- -within 30 min. of waking is 4mg
- take 1 lozenge q1-2h X6weeks, then q2-4h X3weeks, then q4-8h X3 weeks
- depends on alkaline saliva
Nicotrol inhaler
nicotine (Rx only)
- each cartridge is 4mg: max dose/day = 16 cartridges
- -contains enough nicotine for 20 mins. of active puffing
- transmucosal - should not be inhaled into the lungs
Nicoderm CQ
nicotine adhesive matrix system (OTC)
- ind. as an aid to smoking cessation
- strengths: 7mg/24hr, 14mg, 21mg
- apply qday to a clean, hairless dry area on upper outer part of the arm
- -remove after 24hr and apply a new system to a diff. site (do not reuse site for 7 days
- -fold system in half to discard and wash hands after handling
should you smoke while using nicotine products?
no
can you sell nicotine products OTC to people under 18?
no
Nicoderm CQ dosing
>10cigs/day: --21mg X 6 weeks --14mg X 2 weeks --7mg X2 weeks < or equal to 10cigs/day: --14mg X 6 weeks --7mg X 2 weeks
Lidoderm
lidocaine 5% adhesive matrix system
- local anesthetic
- qday
- ind. for pain assoc. with PHN (Herpes zoster and Varicella virus)
- apply up to 3 patches/day at the same time; put on for 12hr then take off for 12hr
- does not contain a PAE
Neurontin
gabapentin
-ind. for PHN and partial
Lyrica
pregabalin
-ind. for PHN, partial, DPN, and fibromyalgia
Varivax
varicella vaccine
- chicken pox vaccine for children or adults
- should not get chicken pox or shingles
Zostavax
zoster vaccine
- only ind. for pts. over 50
- prevents reactivation of varicella virus
Oxytrol
oxybutynin 3.9mg/24hr adhesive matrix system
- anticholinergic = antispasmodic
- BIW
3 main symptoms of OAB
urinary incontinence, urgency, and frequency
micturition
urination
Ditropan XL
oxybutynin ER tablet
-anticholinergic
oxybutynin
IR tablet
Gelnique
oxybutynin 10% topical gel
- anticholinergic
- qday
- individually wrapped packets of gel
- apply to abdomen
- contains a PAE
Detrol
tolterodine IR tablet
- anticholinergic
- ind. for OAB
Detrol LA
tolterodine ER capsule
- anticholinergic
- ind. for OAB
Sanctura
trospium IR tablet
- anticholinergic
- ind. for OAB
- take on ES*
Sanctura XR
trospium ER capsule
- anticholinergic
- ind. for OAB
- take on ES*
Enablex
darifenacin
- anticholinergic
- ind. for OAB
Vesicare
solifenacin
- anticholinergic
- ind. for OAB
Toviaz
fesoterodine
- anticholinergic
- ind. for OAB
side effects of anticholinergics (5)
xerostomia, constipation, sedation, mydriasis, hyperthermia (decreased sweating)
Daytrana
methylphenidate adhesive matrix system (CII)
- ONLY ind. for ADHD (used in children)
- wear on hip 2hr before needed, then take off 9hr later so child will not have trouble sleeping
- strengths: 10mg/9hr, 15mg, 20mg, 30mg
Emsam
selegiline adhesive matrix
- MAOI antidepressant
- only patch ind. for depression
- strengths: 6mg/24hr, 9mg, 12mg
- more centrally active than other MAOIs, so less risk of hypertensive crisis
selegiline pt. counseling
- if taking 9 or 12mg, need to be careful with tyramine
- avoid pseudoephedrine and phenylephrine decongestants
Eldepryl
selegiline ODT
- antiparkinson’s agent
- ONLY ind. for Parkinson’s Disease
Zelapar
selegiline ODT
- antiparkinson’s agent
- ONLY ind. for Parkinson’s Disease
Sancuso
granisetron adhesive matrix 3.1mg/24hr
- antiemetic
- qweek
- ind. for N/V in pts. receiving chemo for 5 straight days (CINV)
- apply on upper arm 24hr before first Tx, take off 24hr after last Tx
- pt. counseling: may cause phototoxic reaction, avoid sun exposure to area patch was applied for 10 days following removal
Aloxi
palonosetron
- antiemetic
- ind. for CINV
Anzemet
dolasetron
- antiemetic
- ind. for CINV
Zofran
ondansetron
- antiemetic
- ind. for CINV
Emend
aprepitant
- antiemetic
- ind. for CINV
Exelon Patch
rivastigmine adhesive matrix system
- cholinesterase inhibitor
- ind. for Alzheimer’s Disease
- start on 4.6mg/24hr for one month, then increase to 9.5mg/24hr
- apply patch to middle of the back so pt. will not remove
- main SE: N/V
Aricept
donepezil
-cholinesterase inhibitor
Razadyne
galantamine
-cholinesterase inhibitor
Butrans
buprenorphine adhesive matrix
- opioid analgesic
- strengths: 5mcg/24hr, 10mcg, 20mcg
- -only use 10, 20mcg in opioid tolerant pts.
- once patch is removed, do not use the same skin site for 3 weeks
- also comes in sublingual tablet: ind. for addiction
- parenteral - Buprenex
Flector
diclofenac epolamine 1.3% adhesive matrix
- NSAID
- ind. for pain due to strains, sprains, and bruises
- BID
- if allergic to aspirin, do not use Flector
strain
muscle stretched too far
sprain
ligament stretched too far
Estrace
estradiol 0.1mg/g cream
- ind. for VA
- applicator calibrated in 1g increments up to 4g
Myrbetriq
mirabegron
-Beta-3 agonist
