Midazolam Hydrochloride Syrup

DRUG DESCRIPTION

Midazolam is a benzodiazepine available as midazolam HCI syrup for oral administration. Midazolam, a white to light yellow crystalline compound, is insoluble in water, but can be solubilized in aqueous solutions by formation of the hydrochloride salt in situ under acidic conditions. Chemically, midazolam HCI is 8-chloro-6-(2-fluo-rophenyl)-1-methyl-4H-imidazo[1,5-a][1,4] benzodiazepine hydrochloride.Midazolam hydrochloride has the molecular formula C18H13CIFN3•HCI, a calculated molecular weight of 362.25 and the following structural formula:

MIDAZOLAM HYDROCHLORIDE  Structural Formula Illustration

Each mL of the syrup contains midazolam hydrochloride equivalent to 2 mg midazolam compounded with artificial bitterness modifier, citric acid anhydrous, D&C Red #33, edetate disodium, glycerin, mixed fruit flavor, sodium benzoate, sodium citrate, sorbitol, and water; the pH is adjusted to 2.8 - 3.6 with hydrochloric acid.

Under the acidic conditions required to solubilize midazolam in the syrup, midazolam is present as an equilibrium mixture (shown below) of the closed ring form shown above and an open-ring structure formed by the acid-catalyzed ring opening of the 4,5-double bond of the diazepine ring.The amount of open-ring form is dependent upon the pH of the solution.At the specified pH of the syrup, the solution may contain up to about 40% of the open-ring compound.At the physiologic conditions under which the product is absorbed (pH of 5 to 8) into the systemic circulation, any open-ring form present reverts to the physiologically active, lipophilic, closed-ring form (midazolam) and is absorbed as such.

 

The following chart plots the percentage of midazolam present as the open-ring form as a function of pH in aqueous solutions.As indicated in the graph, the amount of open-ring compound present in solution is sensitive to changes in pH over the pH range specified for the product: 2.8 to 3.6.Above pH 5, at least 99% of the mixture is present in the closed-ring form.

pH Dependence of Open-ring Form in Water

MIDAZOLAM HYDROCHLORIDE pH Dependence of Open-ring Form in Water Illustration

What are the precautions when taking midazolam hcl syrup (Midazolam Hydrochloride Syrup)?

Before taking midazolam, tell the doctor or pharmacist if you are allergic to it; or to other benzodiazepines (e.g., diazepam); or if you have any other allergies. This product may contain inactive ingredients (such as cherry flavoring), which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: glaucoma (narrow-angle).

Before using this medication, tell the doctor or pharmacist your medical history, especially of: kidney disease, liver disease, breathing problems (e.g., chronic obstructive pulmonary disease-COPD, sleep apnea), heart disease (e.g., congestive heart failure), glaucoma...

Read All Potential Precautions of Midazolam Hydrochloride Syrup »


Midazolam Hydrochloride Syrup Consumer (continued)

SIDE EFFECTS: Nausea, vomiting, dizziness, or drowsiness may occur. If any of these effects persist or worsen, notify the doctor or pharmacist promptly.

Remember that the doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell the doctor immediately if any of these unlikely but serious side effects occur: rapid/slow/shallow breathing, mental/mood changes (e.g., agitation, aggressive behavior), uncontrollable movements (e.g., shaking/tremor), slow/fast heartbeat, vision changes (e.g., blurred vision).

Seek immediate medical attention if any of these rare but very serious side effects occur: fainting, trouble breathing.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact the doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking midazolam, tell the doctor or pharmacist if you are allergic to it; or to other benzodiazepines (e.g., diazepam); or if you have any other allergies. This product may contain inactive ingredients (such as cherry flavoring), which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

This medication should not be used if you have certain medical conditions. Before using this medicine, consult your doctor or pharmacist if you have: glaucoma (narrow-angle).

Before using this medication, tell the doctor or pharmacist your medical history, especially of: kidney disease, liver disease, breathing problems (e.g., chronic obstructive pulmonary disease-COPD, sleep apnea), heart disease (e.g., congestive heart failure), glaucoma (open-angle), personal or family history of regular use/abuse of drugs/alcohol.

This drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Avoid alcoholic beverages.

Before having surgery, tell the doctor or dentist that you are using this medication.

This medication is not recommended for use during pregnancy. It may harm an unborn baby. Infants born to mothers who used similar medications for an extended time have had withdrawal symptoms such as irritability, abnormal/persistent crying, vomiting, or diarrhea. Consult your doctor for more details.

This medication passes into breast milk. Consult your doctor before breast-feeding.



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