dapiprazole

Action and Spectrum

Actions and Spectrum: 

Action: 

dapiprazole’s primary action is to block or inhibit alpha-1 adrenergic receptors. Alpha-1 adrenergic receptors are found in various tissues, including smooth muscles in the eye’s iris and blood vessels. By inhibiting these receptors, dapiprazole reduces the constriction (constriction of blood vessels) of the eye’s iris sphincter muscle and dilates the pupil. This action is helpful in conditions where the constriction of the pupil (miosis) needs to be reversed, such as during eye examinations or certain eye surgeries.  

Spectrum of Use: dapiprazole’s primary use is in the field of ophthalmology. It is specifically employed to reverse the effects of mydriatic and miotic eye drops. Mydriatic eye drops are used to dilate the pupil for eye examinations, while miotic eye drops are used to constrict the pupil. dapiprazole can be used to counteract the pupil-constricting effects of miotic eye drops and restore normal pupil size. 

Drug Interaction

Adverse Reaction

Frequency defined  

Headache (10-40%) 

Browache (10-40%) 

Light sensitivity (10-40%) 

Itchy eyes (10-40%) 

Eye swelling (10-40%) 

Eyelid redness or swelling (10-40%) 

Drooping eyes (10-40%) 

Burning sensation in the eye (about 50%) 

Conjunctival injection (redness of the eye) (over 80%) 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Allergic Reaction: Individuals with known hypersensitivity or allergic reaction to dapiprazole or its components should not use the medication. 

Cardiovascular Conditions: dapiprazole may cause changes in blood pressure and heart rate. Individuals with pre-existing cardiovascular conditions such as heart problems, hypertension (high blood pressure), or arrhythmias (irregular heart rhythms) should be cautious when using dapiprazole. 

Hypertension: dapiprazole can lead to increased blood pressure. Individuals with uncontrolled hypertension should avoid using dapiprazole, or it should be monitored closely under medical supervision. 

Use of Alpha-Blockers: dapiprazole works as an alpha-adrenergic antagonist. Individuals who are already taking alpha-blockers for conditions like benign prostatic hyperplasia (BPH) or hypertension should exercise caution when using dapiprazole, as it can further lower blood pressure. 

Interactions with Other Medications: dapiprazole can interact with other medications, especially those affecting blood pressure, heart rate, or alpha-adrenergic activity. It’s essential to inform your healthcare provider about all your medications before using dapiprazole. 

Pregnancy and Breastfeeding: The safety of dapiprazole during pregnancy and breastfeeding has not been well-established. It’s generally recommended to avoid using dapiprazole during these periods unless the potential benefits outweigh the risks, and under the guidance of a healthcare professional. 

Children: The safety and effectiveness of dapiprazole in pediatric patients may not be fully established. A healthcare provider should carefully consider and monitor its use in children. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

dapiprazole is a medication primarily used in ophthalmology to reverse the effects of mydriatic and cycloplegic drugs, which are substances that dilate the pupils and temporarily paralyze the ciliary muscle in the eye. 

Pharmacodynamics:  

dapiprazole is an alpha-1 adrenergic receptor antagonist. It works by blocking the alpha-1 adrenergic receptors in the iris dilator muscle’s smooth muscle and the eye’s ciliary muscle. This inhibition leads to smooth muscle relaxation, which counteracts the effects of mydriatic and cycloplegic agents, resulting in pupil constriction (miosis) and restoration of average accommodation (cycloplegia reversal).  

Pharmacokinetics: 

Absorption 

dapiprazole is usually administered as eye drops. When applied topically to the eye, it is absorbed through the conjunctiva and the cornea. The systemic absorption is generally low due to the limited penetration of the drug through the eye tissues. 

Distribution 

dapiprazole’s distribution within the body would likely be minimal, given its ophthalmic use. After topical administration, it’s expected to stay primarily localized to the eye tissues. 

Metabolism 

Information about the metabolism of dapiprazole might be limited. Systemic metabolism might not be a significant factor since it is primarily used topically in the eye. Any absorbed drug may undergo metabolism in the liver or other tissues. 

Excretion and Elimination 

Excretion of dapiprazole would likely occur through multiple routes. If the drug is absorbed systemically, it could be excreted primarily through the kidneys, possibly in metabolized or unchanged form. Locally applied drug might also undergo local elimination within the eye tissues. 

Adminstartion

Administration:  

dapiprazole is administered as an eye drop 

Patient Information Leaflet

Patient information leaflet 

Generic Name: dapiprazole 

Why do we use dapiprazole?  

Ophthalmology: dapiprazole is commonly used to reverse the dilation of the pupils that is induced by mydriatic medications (drugs that dilate the pupils) during eye examinations or surgical procedures. After these procedures, it is important to restore normal pupil size to prevent excessive light sensitivity and potential vision disturbances. 

Refraction Testing: dapiprazole can be used to quickly reduce pupil dilation after a refraction test, allowing for more accurate assessment of refractive errors and prescription for corrective lenses. 

Cataract Surgery: dapiprazole may be used after cataract surgery to help return the pupils to their normal size, enhancing patient comfort and vision. 

Posterior Synechiae: Posterior synechiae is a condition where the iris adheres to the lens or cornea of the eye. dapiprazole can be used to break these adhesions and prevent vision problems associated with the condition.