LarkaDrin Capsules

Each LarkaDrin gelatin capsule contains:

Acetaminophen, USP ........................................... 325 mg

Dichloralphenazone, USP .................................... 100 mg

Isometheptene Mucate, USP ................................. 65 mg

Acetaminophen, a non-salicylate, occurs as a white, odorless, crystalline powder, possessing a slightly bitter taste. Acetaminophen is Acetamide, N-(4-hydroxyphenyl)-. It has the following structural formula:

Figure 1: Acetaminophen

C8H9NO2     M.W. 151.16

Dichloralphenazone is a white, microcrystalline powder, with slight odor and tastes saline at first, becoming acrid. It is a mild sedative. Its chemical name is: 1,2-Dihydro-1,5-dimethyl-2-phenyl-3H-pyrazol-3-one, compound with 2,2,2-trichloro-1,1-ethanediol (1:2). Dichloralphenazone has the following structural formula:

Figure 2: Dichloralphenazone

C15H18Cl6N2O5     M.W. 519.07

Isometheptene Mucate is a white crystalline powder having a characteristic aromatic odor and bitter taste. It is an unsaturated aliphatic amine with sympathomimetic properties. Its chemical name is: 6-Methylamino-2-methylheptene, tetrahydroxyadipic acid (2:1) (salt). Isometheptene mucate has the following structural formula:

Figure 3: Isometheptene Mucate

(C9H19N)2•C6H10O8     M.W. 492.65

Inactive ingredients include colloidal silicone dioxide, magnesium stearate, Povidone, sodium laurel sulfate, and starch. The gelatin capsule shells contain gelatin and the following dye systems: Iron Oxide Red, titanium dioxide, and edible printing ink prepared from ingredients conforming to applicable regulations.

Acetaminophen raises the threshold to painful stimuli, thus exerting an analgesic effect against all types of headaches.

Dichloralphenazone, a mild sedative, reduces the patient's emotional reaction to the pain of both vascular and tension headaches.

Isometheptene Mucate, a sympathomimetic amine, acts by constricting dilated cranial and cerebral arterioles, thus reducing the stimuli that lead to vascular headaches.

Transient dizziness and skin rash may appear in hypersensitive patients. This can usually be eliminated by reducing the dose.

Applies to acetaminophen / dichloralphenazone / isometheptene mucate: oral capsule

Applies to acetaminophen / dichloralphenazone / isometheptene mucate: oral capsule

Hypersensitivity

Transient dizziness and skin rash can usually be eliminated by reducing the dose of acetaminophen/dichloralphenazone/isometheptene.[Ref]

Hypersensitivity side effects including transient dizziness and skin rash have been reported with the use of acetaminophen/dichloralphenazone/isometheptene. Hypersensitivity reactions, including anaphylaxis and fixed drug eruptions have been reported rarely in association with acetaminophen use.[Ref]

Hepatic

Alcoholic patients may develop hepatotoxicity after even modest doses of acetaminophen. In healthy patients, approximately 15 grams of acetaminophen is necessary to deplete liver glutathione stores by 70% in a 70 kg person. However, hepatotoxicity has been reported following smaller doses. Glutathione concentrations may be repleted by the antidote N-acetylcysteine. One case report has suggested that hypothermia may also be beneficial in decreasing liver damage during overdose.

In a recent retrospective study of 306 patients admitted for acetaminophen overdose, 6.9% had severe liver injury but all recovered. None of the 306 patients died.

One study has suggested that acetaminophen may precipitate acute biliary pain and cholestasis. The mechanism of this effect may be related to inhibition of prostaglandin and alterations in the regulation of the sphincter of Oddi.

Cases of acute pancreatitis have been reported rarely with the use of acetaminophen.[Ref]

Hepatic side effects including severe and sometimes fatal dose dependent hepatitis have been reported with the use of acetaminophen in alcoholic patients. Hepatotoxicity has been increased during fasting.[Ref]

Gastrointestinal

Gastrointestinal side effects have been rare with the use of acetaminophen except in alcoholics and after overdose.[Ref]

Renal

Renal side effects including acute tubular necrosis and interstitial nephritis have been rare with the use of acetaminophen. Adverse renal effects have been most often observed after overdose, after chronic abuse (often with multiple analgesics), or in association with acetaminophen-related hepatotoxicity.[Ref]

Acute tubular necrosis with acetaminophen use usually occurs in conjunction with liver failure, but has been observed as an isolated finding in rare cases. A possible increase in the risk of renal cell carcinoma has been associated with chronic acetaminophen use as well.

A recent case-control study of patients with end-stage renal disease suggested that long term consumption of acetaminophen may significantly increase the risk of end-stage renal disease particularly in patients taking more than two pills per day.[Ref]

Hematologic

Hematologic side effects including rare cases of thrombocytopenia associated with acetaminophen have been reported. Methemoglobinemia with resulting cyanosis has also been observed in the setting of acute overdose.[Ref]

Dermatologic

Dermatologic side effects including erythematous skin rashes associated with acetaminophen have been reported rarely. Acetaminophen associated bullous erythema and purpura fulminans have also been reported.[Ref]

Respiratory

Respiratory side effects including a case of acetaminophen-induced eosinophilic pneumonia have been reported.[Ref]

Cardiovascular

Cardiovascular side effects including at least two cases of hypotension have been reported following the administration of acetaminophen.[Ref]

Two cases hypotension have been reported following the administration of acetaminophen. Both patients experienced significant decreases in blood pressure. One of the two patients required pressor agents to maintain adequate mean arterial pressures. Neither episode was associated with symptoms of anaphylaxis. Neither patient was rechallenged after resolution of the initial episode.[Ref]

Some side effects of LarkaDrin may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.