Other topical treatment Flashcards
Efudix
Mechansim of Action
Acts as an antimetabolite, binding to thymidylate synthase through the cofactor 5,10- methylene
tetrahydrofolate.
As a result, the enzyme is inhibited and conversion of deoxyuridine to thymidine nucleotides fails, leading to reduced DNA synthesis, a decrease in cell proliferation, and the induction of cell death
Efudix
What is the absorption of the topical dose?
~ 5.98% of a topical dose
What are the contraindications to efudix?
Dihydropyrimidine dehydrogenase (DPD) deficiency
Hypersensitivity to 5 - FU or excipients
Pregnancy (D)
**Precautions with Effudix **
Treatment of the peri-orall or nasolabial area
UVR occlusion
Occlusion
5 - FU pregnancy and lactation advice
AVOID. Cat D
What are the adverse effects of 5-FU
Common (>1%)
- Application site reactions (e.g. local pain, itch, burning, stinging, crusting, weeping, allergic contact
dermatitis, photosensitivity)
Infrequent (0.1–1%)
- Hyper ‑ or hypopigmentation, scarring
Effudix dosing advice
The treatment area at any time should not exceed 500 cm2.
Actinic keratoses
- Apply 1 or 2 times daily. Continue treatment until there is a marked inflammatory response. Initial course of therapy is usually 3 - 4 weeks but may be longer.
- Lesions on the face usually respond quicker than those on the trunk, lower limbs, hands or forearms.
- 70% clearance at 6 months 78% at 12 months
Bowen’s disease
- Apply twice daily for at least 6 weeks. Consider using an occlusive dressing.
Superficial basal cell carcinoma
- Apply to lesions twice daily for 3 - 6 weeks, may continue up to 10 - 12 weeks
How do you manage local skin reactions with Effudix?
Stop Efudix
Cold compress
Paracetamol
Emollient e.g. emulsifying ointment
If severe, consider topical corticosteroid e.g. Advantan ointment daily for 1 week
How does Aldara work?
Synthetic imidazoquinoline amine
Imiquimod mainly acts upon Toll ike receptors (TLRs) that are located on the surface of antigen presenting cells (dendritic cells, monocytes/macrophages, and Langerhans cells).
It is potent TLR- 7 and -8 agonist, leading to activation of a central transcription factor, nuclear factor kappa B (NF-kB). Stimulation of TLR mediated signaling pathways results in the production and release of several endogenous cytokines and chemokines, such as tumor necrosis factor alfa (TNF
a), interferon gamma and alpha, interleukins, granulocyte macrophage colony stimulating factor,
and granulocyte colony stimulating factor.
They, in turn, stimulate both innate and acquired immune response pathways resulting in IQ antitumor activity.
Up to 5% patients do not respond to Aldara due to TLR7 gene mutation/absence
PBS indications for Aldara
(And non PBS)
- Solar keratoses:
- Patient must require topical drug therapy on the face and scalp as field treatment for clinically visible and subclinical lesions where other standard treatments are inappropriate. - sBCC
- The condition must be previously untreated,
- The condition must be confirmed by biopsy,
- Patient must have normal immune function,
- The condition must not be suitable for treatment with surgical excision; OR
- The condition must not be suitable for treatment with cryotherapy; OR
- The condition must not be suitable for treatment with curettage with diathermy, AND
- Patient must require topical drug therapy.
Non - PBS:
- Peri anal or genital condyloma-lata
- Lentigo maligna
Adverse effects of Imiquimod
- Local skin reaction
- Erythema
- Oedema
- Induration
- Irritation
- Flaking/ scaling
- Scabbing/ crusting, erosion/ ulceration
- Pruritus/ itching
- Burning
- Papules
- Vesicles
- Hyper/ hypopigmentation
- Alopecia
- Fatigue
- Flu-like symptoms
- Infection
- GI upset
- Anorexia
- Arthralgia
- Myalgia
- Back pain
- Headache
- Autoimmune disease exacerbation e.g. psoriasis (rare)
- Erythema multiforme
- Stevens-Johnson syndrome
What % strenght is imiquimod?
5%
What is the dosing schedule for imiquimod?
Actinic keratosis
Cyclical
3x/week (M/W/F) for 4 weeks; stop for 4 weeks & then reassess; may repeat for a further 4 weeks
Continuous
3x/week (M/W/F) for up to 16 weeks
Up to 25cm2
Superficial basal cell carcinoma
5x/week (M -F) for 6 weeks
Apply 1cm around tumour
Assess response 6 - 12 weeks after cessation of treatment
Treatment area should not exceed 25cm
2
(5x5cm)
Condyloma accuminatum - external
3x/week up to 16 weeks at bed time,
leave on skin for 6 to 10 hours.
Do not occlude
Lentigo maligna
5x/week
for 12 weeks (60 applications)
What is Picato?
Include Mechanism of action
A topical agent for the treatment of actinic keratoses
Ingenol mebutate gel is a protein kinase C activator fro Euphorbia peplus
- (1) Induction of local lesion cell death;
- (2) promotion of an inflammatory response characterised by local production of proinflammatory cytokines and chemokines and infiltration of immunocompetent cells.
- $134.99
What is the dosing of Picato?
Actinic keratosis, Face and Scalp
* Apply 0.015% gel topically to affected area once daily for 3 consecutive days; allow to dry for 15 minutes; avoid touching or washing area for 6 hours after application.
Actinic keratosis, Trunk and Extremities
* Apply 0.05% gel topically to affected area once daily for 2 consecutive days; allow to dry for 15 minutes; avoid touching or washing area for 6 hours after application.
Adverse effects of Picato
Common (>1%)
- Application site reactions (eg pain, erythema, crusting, swelling, blisters, ulceration, pustules, infrequently paraesthesia), periorbital or eyelid oedema (may be due to spreading of swelling from the application site)
Rare (<0.1%)
- Allergic reactions (including anaphylaxis, angioedema, rashes and allergic contact dermatitis)
How do you apply Picato?
- Do not apply immediately before or after taking a shower or less than 2 hours before bedtime.
- Squeeze the gel from the single use tube onto fingertip
- Spread it evenly over treatment area and allow dry for 15 minutes
- Do not cover
- Wash hands after
- Leave for 6 hours and then wash off with mild soap and water .
- Optimal therapeutic effect can be assessed approximately 8 weeks after treatment
What is Solaraze?
What is the MoA
What do we use it for in derm?
- Diclofenac sodium 3% gel, 25g $58.39
- Unknown for AK - inhibition of the cyclooxygenase pathway leading to reduced prostaglandin E2 (PGE2) synthesis. COX2
Treatment of AKs
What is the dosing for Solaraze?
- BD for 60-90 days, 30 days to heal
- Max 8g daily
- 0.5g for 5x5cm2
What is the pregancy classification of solaraze?
- Pregnancy category C
- Not to BF
What is hydroquinone?
What is it used for in Dermatology?
MoA?
Strength?
A skin lightening agent
MoA: reduces pigmentation by competing with tyrosine as a substrate for tyrosinase resulting in selective damage to melanosomes and melanocytes (via ROS)
2%, 3% and 4%
Can you use hydroquinone in pregnancy?
Lack of studies - best avoid
What are the key keratolytic agents?
Sal acid
