Alcaftadine

Alcaftadine

Systematic (IUPAC) name
2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0(3,7)]tetradeca- 1(14),3,5,10,12-pentaene-6-carbaldehyde
Clinical data
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a611022
Licence data	US FDA:link
Pregnancy category	US: B (No risk in non-human studies)
Legal status	US: ℞-only
Routes of administration	Topical
Pharmacokinetic data
Biological half-life	~2 hrs
Identifiers
CAS Number	147084-10-4 N
ATC code	S01GX11
PubChem	CID 19371515
IUPHAR/BPS	7587
DrugBank	DB06766 Y
ChemSpider	14201635 Y
UNII	7Z8O94ECSX Y
KEGG	D06552 N
ChEBI	CHEBI:71023 N
ChEMBL	CHEMBL1201747 N
Chemical data
Formula	C19H21N3O
Molar mass	307.40 g·mol−1
SMILES CN1CCC(=C2c3ccccc3CCn4c(C=O)cnc24)CC1
NY (what is this?)  (verify)

Alcaftadine is used to prevent eye irritation brought on by allergic conjunctivitis. It is a H1 histamine receptor antagonist.^[1]

It was approved by the U.S. Food and Drug Administration in 2010 under the trade name Lastacaft.

Pharmacology

Alcaftadine is an antagonist at three of the histamine receptors (1, 2 and 4). The main indication for Alcaftadine is for prevention of allergic conjunctivitis. By blocking these four receptors, Alcaftadine has been shown to significantly reduce the effects of allergens. This effect on histamine receptors seems to show lower rates of itching, eosinophil recruitment and redness after exposure to an allergen.^[2] The effect of alcaftadine seemed to reduce the amount of eosinophil cells significantly as compared to olopatadine 0.1%. When animal models were used to test alcaftadine, alcaftadine 0.25% seemed to show superior results for decreasing E-cadherin expression as compared to placebo. The reduction of E-cadherin means decreased junctions which would lead to progression of allergic conjunctivitis.^[3]

Clinical relevance

When Alcaftadine was tested against placebo and olopatadine, only Alcaftadine 0.25% was shown to have a clinically significant reduction in conjunctival redness scores 7 and 15 minutes after administration. When clinical groups where compared to placebo, treatment with all three of the alcaftadine groups (0.05, 0.1 and 0.25%) showed a reduction in secondary endpoints of (lid swelling, conjunctival redness, ocular itching/tearing) as compared to placebo.^[2]

Adverse effects

In studies comparing the effectiveness of olopatadine to alcaftadine, there was not a dose response increase of adverse effects as alcaftadine doses increases for 0.05% to 0.1% to 0.25%. The most common seen side effect of alcaftadine administration was irritation or a stinging sensation at the administration site.^[2]

Pharmacokinetics

Alcaftadine is typically administrated as an eye drop which keeps its effects regional as compared to systemic effects. The main metabolite of alcaftadine is a carboxylic acid metabolite that has minimal systemic effects. The maximum concentration of its main active metabolite is 0.06ng/ml at Tmax of 15 minutes. The minimal absorption of alcaftadine, leads to minimal systemic accumulation. The half life of the major metabolite of alcaftadine is two hours after ocular administration. Except for the metabolite, the rest of alcaftadine is excreted unchanged. Since alcaftadine is administrated at a small concentration and at a local site (the eye), it seems to have minimal systemic effects.^[4]

Sales

Sales for Alcaftadine from the company Allergan began in July of 2010. Since the beginning of sales, Alcaftadine prescriptions have increased until at least March of 2012. From the time period of July 2010 until March 2012, cumulative sales have reached 139,000 prescriptions. Out of these 139,000 prescriptions there have been 104,000 unique patients. In March of 2012, Alcaftadine exceeded sales of Elestat and this trend may continue as prescribers see the benefit of Alcaftadine and become more comfortable prescribing it.^[5]

See also

• Ketotifen

References

External links

• Alcaftadine and Tacrolimus pharmacological studies for Allergic Conjunctivitis.