Capellon.com

Tekral Tablets
NDC 64543-025-90

DESCRIPTION
Each light yellow and light green bi-layered capsule shaped tablet that is scored on one side
and debossed “TEKRAL” on the opposite side contains:
Diphenhydramine
Hydrochloride . 100 mg
Pseudoephedrine
Hydrochloride ………. 120 mg
Tekral tablets are specially formulated to provide prolonged activity and contain active
ingredients of the following therapeutic classes: antihistamine and nasal decongestant.
Inactive ingredients include: calcium phosphate dibasic, colloidal silicon dioxide, D&C
Yellow #10, Green Lake blend green dye, lactose monohydrate, magnesium stearate (veg.),
methylcellulose, microcrystalline cellulose, povidone and stearic acid.
Diphenhydramine Hydrochloride is an antihistamine having the chemical name,
Ethanamine, 2-(diphenylmethoxy)-N,N-dimethyl-, hydrochloride. The chemical structure of
Diphenhydramine Hydrochloride is as follows:
C17H21NO • HCl M.W. 291.82 Pseudoephedrine hydrochloride is a Benzenemethanol, α-[1- (methylamino)ethyl]-,[S- (R*,R*)]-, hydrochloride. It has the following chemical structure: C10H15NO • HCl M.W. 201.69 CLINICAL PHARMACOLOGY
Diphenhydramine hydrochloride is an antihistamine with anticholinergic (drying) and
sedative side effects. Antihistamines appear to compete with histamine for cell receptor
sites on effector cells. Diphenhydramine hydrochloride is widely distributed throughout the
body, including the CNS. A portion of the drug is excreted unchanged in the urine, while the
rest is metabolized via the liver.
Pseudoephedrine hydrochloride is a sympathomimetic which acts predominately on alpha
receptors and has little effect on beta receptors. Because of this selective activity, it
functions as a nasal decongestant with minimal CNS stimulation although the latter is
known to occur in some instances.
INDICATIONS AND USAGE
Tekral tablets are indicated for the temporary relief of symptoms associated with seasonal
and perennial allergic rhinitis and vasomotor rhinitis, including nasal congestion.
CONTRAINDICATIONS
This product is contraindicated in patients with hypersensitivity to antihistamines or
sympathomimetic amines, in nursing mothers, in infants and in patients receiving
monoamine oxidase inhibitor (MAOI) therapy (see Drug Interactions section) or in patients
with narrow angle glaucoma, urinary retention, peptic ulcer and during an asthmatic attack.
Sympathomimetic amines are contraindicated in patients with severe hypertension or
severe coronary artery disease.
WARNINGS
Caution should be exercised in patients with stenosing peptic ulcer, pyloroduodenal
obstruction, or bladder-neck obstruction, hypertension, diabetes mellitus, ischemic heart
diseases, hyperthyroidism, increased intraocular pressure narrow angle glaucoma and
prostatic hypertrophy. Patients sixty (60) years and older may demonstrate an increased
response to this drug combination, both in therapeutic effect and in the incidence of adverse
reactions and hence a lower dose may be more appropriate for these patients.
Antihistamines and/or decongestants may cause excitability particularly in children. At
doses higher than the recommended dose, nervousness, dizziness or sleeplessness may
occur.
PRECAUTIONS
General: Preparations containing pseudoephedrine should be used with caution in the
presence of hypertension; coronary artery disease; any other cardiovascular disease;
glaucoma; prostatic hypertrophy; hyperthyroidism; diabetes. Antihistamines have an
atropine-like action and, therefore, should be used with caution in patients with a history of
bronchial asthma, increased intraocular pressure, hyperthyroidism, cardiovascular disease
and hypertension.
Information for Patients: Patient consultation should include the following information
regarding proper use of this medication:
• Do not take more medication than the amount recommended.
• Take medication with food, water, or milk to minimize gastric irritation.
• Swallow extended release dosages whole.
• Do not drive or operate machinery if drowsiness or dizziness occurs.
• Do not ingest alcoholic beverages, monoamine oxidase inhibitors, or CNS
depression-producing medications (hypnotics, sedatives, tranquilizers) while taking this
medication.
• If a dose is missed, the medication should be taken as soon as possible unless it is almost
time for the next dose. Do not double doses.
• This medication should be stored in a tight, light-resistant container at temperatures
between
20°- 25°C (68°- 77°F); see USP Controlled Room Temperature.
• Keep all medications out of the reach of children. In case of accidental over dose, seek
professional assistance or contact a poison control center immediately.
Caution patients about the signs of potential side effects, especially:
• Anticholinergic effects-clumsiness or unsteadiness; severe drowsiness; severe dryness of
mouth, nose, or throat; flushing or redness of face; shortness of breath or troubled
breathing.
• Blood dyscrasias – sore throat and fever, unusual bleeding or bruising, unusual tiredness
or weakness.
• Fast or irregular heartbeat.
• Psychotic episodes.
• Tightness in chest.

Drug/Laboratory Test Interactions: Antihistamines may interfere with diagnostic test
results for skin tests using allergen extracts. The in vitro addition of pseudoephedrine to
sera containing the cardiac isoenzyme MB of serum creatine phosphokinase progressively
inhibits the activity of the enzyme. The inhibition becomes complete over six hours.
Drug Interactions: Do not take this product if you are presently taking, or have taken within
the preceding two weeks, a prescription drug for high blood pressure or depression without
first consulting your physician.
• MAOIs and Tricyclic Antidepressants – may prolong and intensify the anticholinergic
(drying) effects of antihistamines. When sympathomimetic drugs are given to patients
receiving MAOIs, hypertensive reactions, including hypertensive crises, may occur.
• CNS Depressants - concomitant use of antihistamines with alcohol, tricyclic
antidepressants, barbiturates and other CNS depressants may have an additive effect.
• Antihypertensives - the antihypertensive effects of guanethidine, methyldopa,
mecamylamine, reserpine, and veratrum alkaloids may be reduced by sympathomimetics.
Beta-adrenergic blocking agents may also interact with sympathomimetics.
• Digitalis – increased ectopic pacemaker activity can occur when pseudoephedrine is used
concomitantly with digitalis.
• Antacids – increase the rate of absorption of pseudoephedrine while kaolin decreases it.

Carcinogenesis, Mutagenesis, Impairment of Fertility: No data are available on the
long-term potential of the components of this product for carcinogenesis, mutagenesis, or
impairment of fertility in animals and humans.
Pregnancy: Teratogenic Effects: Pregnancy Category C. There are no adequate and
well-controlled studies in pregnant women. This product should be used during pregnancy
only if the potential benefits to the mother justify the potential risks to the infant.
Nonteratogenic Effects: Pseudoephedrine passes through the blood-brain and placental
barriers. Antihistamines should not be used in the third trimester of pregnancy because
newborns and premature infants may have severe reactions to them, such as convulsions.

Nursing Mothers: It is not known whether this drug is excreted in human milk. However,
certain antihistamines and sympathomimetics are known to be excreted in human milk.
Because of the higher risks of antihistamines for infants generally, and for newborns and
prematures in particular, a decision should be made whether to discontinue nursing or to
discontinue the drug, taking into account the importance of the drug to the mother. There is
a report of irritability, excessive crying and disturbed sleeping patterns in a nursing infant
whose mother had taken a product containing an antihistamine and pseudoephedrine.
Pediatric Use: Do not give this product to children under 6 years of age except under the
advice and supervision of a physician.
Geriatric Use: Confusion, dizziness, sedation, hypotension, hyperexcitability, and
anticholinergic side effects, such as dryness of mouth and urinary retention (especially in
males), may be more likely to occur in geriatric patients taking antihistamines. Geriatric
patients taking sympathomimetics may be more likely to experience confusion,
hallucinations, seizures and CNS depression. Geriatric patients may also be more sensitive
to the effects, especially to the vasopressor effects of sympathomimetic amines.
Demonstrate safe use of a short-acting antihistamine / sympathomimetic formulation before
use of an extended release formulation in elderly patients.
ADVERSE REACTIONS
The physician should be alert to the possibility of any of the adverse reactions which have
been observed with sympathomimetic and antihistaminic drugs. These include: drowsiness;
confusion,
restlessness, nausea, vomiting, drug rash, vertigo, palpitation, anorexia, dizziness, dysuria
due to vesicle sphincter spasm, headache, insomnia, anxiety, tension, weakness,
tachycardia, angina, sweating, blood pressure elevation, mydriasis, gastric distress,
abdominal cramps, central nervous system stimulation and circulatory collapse.
DRUG ABUSE AND DEPENDENCE
Pseudoephedrine, like other central nervous system stimulants, has been abused. At high
doses, subjects commonly experience an elevation of mood, a sense of increased energy
and alertness and decreased appetite. Some individuals become anxious, irritable and
loquacious. In addition to the marked euphoria, the user can experience a sense of
markedly enhanced physical strength and mental capacity. With continued use, tolerance
develops, the user increases the dose, and toxic signs and symptoms appear. Depression
may follow rapid withdrawal. Stimulants such as pseudoephedrine are banned and tested
for by the U.S. Olympic Committee (USOC) and the National Collegiate Athletic Association
(NCAA).
OVERDOSAGE
Signs and Symptoms: This product is comprised of pharmacologically different
components: an antihistamine and a sympathomimetic amine. Therefore, it is difficult to
predict the exact manifestation of symptoms in a given individual. A description of
symptoms which are likely to appear after ingestion of an excess of the individual
components follows:
Overdosage with antihistamines may cause hallucinations, convulsions or possible death,
especially in infants and children. Antihistamines are more likely to cause dizziness,
sedation and hypotension in elderly patients. Overdosage with sympathomimetic amines
can cause cardiac arrhythmias, cerebral hemorrhage and pulmonary edema. It can also
cause palpitation, tremor, dizziness, vomiting, fear, labored breathing, headache, dryness of
mouth, pallor, weakness, panic, anxiety, confusion, hallucinations and delirium.

Recommended General Treatment: In the event of overdosage, emergency treatment
should be started immediately. Since the action of extended release products may continue
for as long as 12 hours, treatment at overdosage should be directed toward reducing further
absorption and supporting the patient for at least that length of time. Since there is no
specific antidote for overdose with antihistamine and decongestant combinations, treatment
is symptomatic and supportive with possible utilization of the following:
• Induction of emesis (syrup of ipecac recommended); however, precaution against
aspiration is necessary especially in infants and children.
• Gastric lavage (isotonic or 0.45% sodium chloride solution) if patient is unable to vomit
within three hours of ingestion.
• Saline cathartics (milk of magnesia) are sometimes used.
• Vasopressors to treat hypotension; however, epinephrine should not be used since it may
further lower blood pressure.
• Oxygen and intravenous fluid.
• Precaution against the use of stimulants (analeptic agents) is recommended because they
may cause seizures.
• Short-acting barbiturates, diazepam or paraldehyde may be administered to control
seizures.
• Hyperpyrexia, especially in children, may require treatment by means of external cooling.
• Apnea is treated with ventilatory support.
DOSAGE AND ADMINISTRATION
Adults and children over 12 years of age: One tablet every 12 hours. Not to exceed 2 in
24 hours.
Children 6 to 12 years of age: As prescribed by physician.
Children under 6 years of age: Do not give this product to children under 6 years of age
except under the advice and supervision of a physician.
HOW SUPPLIED
Tekral tablets are supplied as light green and light yellow bi-layered capsule shaped tablets
with "TEKRAL" debossed on one side of the tablet, and scored on the opposite side.
Available in bottles of 90 tablets (NDC 64543-025-90), and physician samples of 2 tablet
blister packs, NDC 64543-025-02.
KEEP THIS AND ALL MEDICATION OUT OF THE REACH OF CHILDREN. IN CASE OF
ACCIDENTAL OVERDOSE, SEEK PROFESSIONAL ASSISTANCE OR CONTACT A
POISON CONTROL CENTER IMMEDIATELY.
Dispense in tight, light-resistant containers as defined in the USP/NF with child-resistant
closures.
Store at controlled room temperature 20°- 25°C (68°- 77°F); see USP Controlled Room
Temperature.
Rx Only
Distributed by:
Capellon Pharmaceuticals, Ltd.
Fort Worth, TX 76118
500385 Iss. 07/09

Source: http://www.capellon.com/PI/TekralPI.pdf