COMPOSITON
ACTIVE – P TAB
Each tablet contains
Triprolidine HCl 5mg
Phenylephrine HCl 10mg
Paracetamol 500mg
INTRODUCTION
ACTIVE-P containing Paracetamol 500mg, Triprolidine HCL 5 mg and Phenylephrine
10 mg is used to treat nasal congestion; itchy, watery eyes; itchy throat;
sneezing; headache; fever; and other symptoms associated with allergies, hay
fever , and the common cold.
Triprolidine is an antihistamine. It blocks the effects of the
naturally occurring chemical histamine in the body. Triprolidine prevents
sneezing; itchy, watery eyes and nose; and other symptoms of allergies and hay
fever. Antihistamines are used to relieve or prevent the symptoms of hay fever
and other types of allergy. They may also help relieve some symptoms of the
common cold, such as sneezing and runny nose. They work by preventing the
effects of a substance called histamine, which is produced by the body.
Pseudoephedrine is a vasoconstrictor decongestant. It constricts
blood vessels. This reduces the blood flow to certain areas, which decreases
swelling and allows nasal and respiratory passages to open up. Decongestants,
such as Phenylephrine, produce a
narrowing of blood vessels. This leads to clearing of nasal congestion, but it
may also cause an increase in blood pressure in patients who have hypertension.
Paracetamol is an analgesic, antipyretic and anti-inflammatory
agent. Analgesics, such as Paracetamol and salicylates (e.g., aspirin, sodium
salicylate), are used in these combination medicines to help relieve fever,
headache, aches, and pain.
PHARMACOLIGY
Pharmacodynamics
The drug may directly stimulate
adrenergic receptors but probably indirectly stimulates both a and b adrenergic
receptors by releasing norepinephrine from its storage sites. Pseudoephedrine
increases heart rate, force of contraction and cardiac output, and
excitability. It acts on a receptors in the mucosa of the respiratory tract,
producing vasoconstriction which results in shrinkage of swollen mucous
membranes, reduction of tissue, hyperemia, edema and nasal congestion, and an
increase in nasal airway potency. Pseudoephedrine causes CNS stimulation and
reportedly has an anorexigenic effect.
Triprolidine blocks the effects
of the naturally occurring chemical histamine in the body, thereby relieving
the allergic symptoms. Paracetamol relieves pain and fever by blocking the
Prostaglandin (PG) secretion to the site of pain.
Pharmacokinetics
Triprolidine is absorbed from the
GI tract and metabolized into a caboxylated derivative. It is excreted mainly
in urine.
Phenylephrine has low oral
bioavailability owing to irregular absorption and first-pass metabolism by
monoamine oxidase in the gut and liver.
Paracetamol is readily absorbed
from the GI tract with peak plasma concentration occurring about 10-16 minutes
after oral administration. It is distributed into most body tissues, crosses
the placenta and is present in breast milk. It is metabolized primarily in liver
and excreted in urine. Less than 5% is excreted as unchanged Paracetamol.
DOSE AND ADMINISTRATION
Dose should be taken as directed
by the physician. Each dose should be swallowed whole with a full glass of
water. The maximum amount of paracetamol for adults is 1 gm (1000 mg) per dose
and 4 gm (4000 mg) per day. Taking more paracetamol could damage liver. Active-P should not be used for more
than 7 to 10 days in a row.
CONTRAINDICATIONS
Hepatic damage, peptic ulcer and
hypersensitivity.
DRUG INTERACTIONS
Active-P may increase the effects of other drugs that cause drowsiness, including
antidepressants, alcohol, other antihistamines, pain reliever, anxiety
medicines, seizure medicines, and muscle relaxants. Dangerous sedation,
dizziness, or drowsiness may occur if Active-P
is taken with any of these medications.
ACTIVE-P has drug interaction with monoamine oxide inhibitor
(MAOI). A very serious drug interaction could occur, leading to serious side
effects.
ADVERSE REACTIONS
Liver damage, blood problems (easy
or unusual bleeding or bruising) or low blood sugar, Dry eyes, nose, and mouth
drowsiness or dizziness blurred vision difficulty urinating; or; excitation in
children.
PRECAUTIONS
ACTIVE-P may cause dizziness or drowsiness so precaution should be
taken when driving, operating machinery, or performing other hazardous
activities.
Alcohol may increase drowsiness
and dizziness while taking ACTIVE-P. Alcohol
may also cause damage to liver when taken with Paracetamol.
Safety in pregnancy is not established.
ACTIVE-P may in traces metabolized through breast milk.
OVERDOSAGE
Symptoms of an ACTIVE-P overdose include a dry mouth,
large pupils, flushing, nausea, vomiting, abdominal pain, diarrhea, seizures,
confusion, sweating, and an irregular heartbeat.
