Clomin: (Dicyclomine HCL & Paracetamol)

Clomin is composed of Dicyclomine HCL & Paracetamol with the ratio of Dicylomine HCL B.P. 20 mg and Paracetamol I. P. 500mg and, it is meant for oral administration.

CHEMISTRY OF DICYCLOMINE

Molecular Formula: 2-Diethylaminoethyl bicyclohexyl – 1 Carboxylate hydrochloride.

Structure: C19H35NO2HCL (The compound is official in B.P. & U.S.P.)

Physical Properties:

  • Molecular Weight: 346
  • Description: White odourless crystalline powder.
  • Solubility: Soluble in water, alcohol, and chloroform.
  • Taste: Bitter numbing taste.
  • PHARMACOKINETICS OF DICYCLOMINE

    Absorption: Dicyclomine is absorbed from g.i. tract after administration. Being a tertiary amine, it can pass through physiological membranes easily.

    Distribution: Dicyclomine has its pharmacological action upto the urinary tract but it is not known whether this effect is due to Dicyclomine or its metabolites. It is also known as whether the effect is due to active ingredient reaching in urinary tract or due to its concentration in blood.

    Metabolism: the major site of metabolism seems to be liver. However, possibility of drug being excreted largely as unchanged Dicyclomine cannot be ruled out. Elimination: Mainly through faeces & urine.

    PHARMACODYNAMICS OF DICYCLOMINE

    Dicyclomine is a relatively new antispasmodic agent belonging to the class of anticholinergic agents. It also has a potent smooth muscle relaxing effect not attributable to its antimuscarinic (anticholingergic) property. Further, it also decrease spasm of gastrointestinal tract, biliary tract, ureter, and uterus without producing characteristic atropine effects on the salivary, sweat, or gastrointestinal glands, the eye, or the cardiovascular system, except in large doses .

    Moreover, the major action of Dicyclomine is purported to be a non-specific direct relaxant action on smooth muscle rather than a competitive antagonism of the spasm of gastrointestinal smooth muscle induced experimentally by a variety of spasmogens, viz acetycholine, barium chloride, urea, histamine and bradykinin.

    CHEMISTRY OF PARACETAMOL

    Paracetamol is known as Acetaminophen in U.S.P.
    Molecular Formula:
    n-acetyl-p-amino phenol

    Structure: C8H9NO2

    Physical Properties:

  • Molecular Weight: 151.2
  • Description: It is white odourless crystalline powder.
  • Solubility: Soluble in water, alcohol, and acetone.
  • Taste: Bitter taste.
  • PHARMACOKINETICS OF PARACETAMOL

    Absorption: Paracetamol is readily absorbed from the g.i. tract. It is also absorbed from rectum when administered in a form of suppository.

    Distribution: After oral administration, peak plasma concentration is achieved in 30 m. to 2 hours. The elimination half-life varies from about 1 to 4 hours. Plasma protein binding of Paracetamol is negligible at therapeutic doses but it is more if the dose is increased. It is uniformly distributed in all body fluids.

    Metabolism: It is metabolised in liver and is converted into glucuronide and sulphate conjugates.

    Excretion: Paracetamol mainly excreted through kidney as glucuronide & sulphate.

    PHARMACODYNAMICS OF PARACETAMOL

    Paracetamol has analgesic and antipyretic effects which do not differ significantly from those of aspirin. It also has very weak anti-inflammatory effect.

    Mechanism of action: Paracetamol is a weak inhibitor of prostaglandin biosynthesis in periphery and that is probably the reason of its weak anti-inflammatory action. However, it has been shown to have an inhibitory effect on central prostaglandin synthesis. Paracetamol thereby prevents prostaglandin synthesis in CNS and prostaglandin is pain transmitter in CNS. It may therefore have its analgesic action center in nature.

    When applied in very minute quantities to thermoregulatory centers in brain, Paracetamol reduces body temperature significantly. However, peripheral component of antipyretic effect like vasodilatation is also present.

    MEDICAL USES

    Clomin is being used to treat various problems such as:

  • Gastro-intestinal spasm: Dicyclomine is used clinically for the relief of gastrointestinal spasm. Besides, it is helpful as spasmolytic in irritable bowel.
  • Un-inhibited bladder syndrome: Dicyclomine is being mainly a direct acting antispasmodic agent; it is useful in the treatment of small contracted bladder or uninhibited bladder syndrome. Pain radiates to back muscles. Paracetamol is useful in pain and muscle spasm associated with this syndrome.
  • Spasm of Ureter: Dicyclomine relieves spasm of ureter. Hence it is useful in clinical management of rental colic.
  • Biliary tract spasm: Dicyclomine relieves spasm of biliary tract; hence it relieves pain of biliary colic. Paracetamol relieves associated problems.
  • Uterine Spasm: Dicyclomine relieves spasm of uterus. This makes it useful in treatment of uterine spasmodic conditions including spasmodic dysmenorrhea. Paracetamol serves as a safe analgesic.
  • PRECAUTIONS

    Preparation with Dicyclomine should be a administered with caution in patients over the age of 40 as it may precipitate an attack of acute congestive glaucoma.

    Care should be taken in patients with enlarged prostate as retention of urine may develop.

    It should be also given with caution to chronic lung patients.

    Caution should be observed in the cases of congestive cardiac failure, tachycardia and pyloric obstruction.

    Paracetamol should be given with care in the case of impaired liver or kidney damage.

    Clomin should be avoided during pregnancy.

    OVERDOSE

    Overdose of Clomin will show atropinic side effects as first symptoms. Immediate hospitalization is essential as toxic doses may cause respiratory depression.