Dosing and uses of Aldara, Zyclara (imiquimod)
Adult dosage forms and strengths
topical cream
- 2.5% (Zyclara)
- 3.75% (Zyclara)
- 5% (Aldara)
Actinic Keratosis
Indicated for topical treatment of clinically typical, nonhyperkeratotic, nonhypertrophic actinic keratoses on the face or scalp in immunocompetent adults
Zyclara 2.5% or 3.75%: Apply qDay to skin of affected area (either entire face or balding scalp) for two 2-week treatment cycles separated by 2-week no-treatment period
Aldara 5%: Apply 2 times a week for 16 weeks to one defined treatment area (contiguous area <25 cm²); examples of dosing schedules include Monday and Thursday or Tuesday and Friday
Superficial Basal Cell Carcinoma
Target tumor should have maximum <2 cm diameter and be located on trunk (excluding anogenital skin), neck, or extremities (excluding hands and feet); treatment area should include 1 cm margin of skin around tumor
Aldara 5%: Apply 5 times a week for 6 weeks to biopsy-confirmed superficial basal cell carcinoma and include 1 cm margin of skin around tumor
External Genital Warts
Indicated for the treatment of external genital and perianal warts/condyloma acuminata
Zyclara 3.75%: Apply as thin film to entire treatment area and rub in until cream is no longer visible; may wash with mild soap and water after 8 hours of application; use 1 packet or 1 full actuation of pump
Aldara 5%: Apply 3 times a week until total clearance of warts or for a maximum of 16 weeks; examples of application schedules are Monday, Wednesday, Friday or Tuesday, Thursday, Saturday; use 1 packet only for each application
Bladder Cancer (Orphan)
Orphan designation for treatment of carcinoma in situ of the urinary bladder
Sponsor
- Telormedix SA; Via della Posta 10, CH-6934 Bioggio; SWITZERLAND
Dosing Considerations
Zyclara can be used daily on larger surface areas than Aldara
Actinic keratosis: Do not extend specified treatment cycle due to missed doses or rest periods
Administration
External genital warts: Apply prior to normal sleeping hours and leave on skin for approximately 6-10 hr; then wash with mild soap and water; nonocclusive dressings such as cotton gauze/underwear may be used in management of skin reactions
Do not bandage application area
Wash hands before and after application
Zyclara Pump: Prime before first use only by repeatedly depressing actuator until cream is dispensed
Avoid use in or on lips, nostrils or eyes
Pediatric dosage forms and strengths
topical cream
- 3.75% (Zyclara)
- 5% (Aldara)
External Genital Warts
Indicated for the treatment of external genital and perianal warts/condyloma acuminata
<12 years: Safety and efficacy not established
≥12 years
- Zyclara 3.75%: Apply as thin film to entire treatment area and rub in until cream is no longer visible; may wash with mild soap and water after 8 hours of application; use 1 packet or 1 full actuation of pump
- Aldara (5%): Apply 3 times a week until total clearance of warts or for a maximum of 16 weeks; examples of application schedules are Monday, Wednesday, Friday or Tuesday, Thursday, Saturday; use 1 packet only for each application
Administration
External genital warts: Apply prior to normal sleeping hours and leave on skin for approximately 8 hr; then wash with mild soap and water; non-occlusive dressings such as cotton gauze/underwear may be used in management of skin reactions
Aldara, Zyclara (imiquimod) adverse (side) effects
>10%
Application site reaction (33%)
URTI (15%)
Erythema (54-61%)
Erosion (29-31%)
Excoriation/flaking (18-25%)
Edema (12-17%)
Itching (20%)
1-10%
Sinusitis (7%)
Burning (6%)
Headache (5%)
Carcinoma squamous (4%)
Diarrhea (3%)
Bleeding (3%)
Stinging (3%)
Pain (3%)
Eczema (2%)
Induration (2%)
Tenderness (2%)
Irritation (2%)
Back pain (1%)
Fatigue (1%)
Atrial fibrillation (1%)
Viral infection (1%)
Dizziness (1%)
Vomiting (1%)
UTI (1%)
Fever (1%)
Rigor (1%)
Alopecia (1%)
Frequency not defined
Headache
Flu-like symptoms
Myalgia
Warnings
Contraindications
None
Cautions
Avoid or minimize exposure to sunlight, including sunlamps; wear protective clothing
Do not use until skin has fully healed from previous drug or surgical treatment
Avoid use in patients with pre-existing autoimmune conditions
Safety and efficacy not established for other forms of BCC besides sBCC Safety and efficacy not established for sBCC lesions on head, face or anogenital area
Dosage is different for different indications
Avoid sexual contact while cream is on skin
Aldara: Safety when applied to skin area >252 cm in treatment of actinic keratosis have not been determined
Intense local skin reactions including skin weeping or erosion may occur after few applications; may require interruption of dosing
May exacerbate inflammatory skin conditions such as chronic graft versus host disease
Severe local inflammatory reactions of female external genitalia can lead to severe vulvar swelling, which may lead to urinary retention; dosing should be interrupted or discontinued
A transient increase in lesion counts may be observed during treatment
Not recommended for oral, ophtalmic, urethral, intravaginal, cervical, rectal, or intra-anal human papilloma viral disease
Do not use in children aged 2-12 years with molluscum contagiosum due to studies failing to demonstrate efficacy
Safety and efficacy not established in immunosuppressed patients or those with basal cell nevus syndrome or xeroderma pigmentosum
Caution in patients with pre-existing autoimmune conditions
Flu-like signs and symptoms may accompany or precede local skin reactions (eg, fatigue, fever, nausea, malaise, arthralgias, chills); interrupt treatment and reassess
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown if distributed in breast milk; use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Aldara, Zyclara (imiquimod)
Mechanism of action
Unknown mechanism in treating actinic keratosis and external genital warts; immune response modifier, stimulates release of inflammatory cytokines and proliferation/migration of immune cells
No direct antiviral activity
Absorption
Appears to be dependent on area of application rather than amount applied
Peak plasma concentration (Aldara): 0.1-3.5 ng/mL
Peak plasma concentration (Zyclara): 0.323 ng/mL
Elimination
Excretion: Urine
