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Drugs
Drugs
[Croma Medic]
Dosage: 1 tab daily for the first 4-7 days, increased by the same amount once
a week until a maintenance dose of 1-3 tab/s bid. Max 600mg/day.
Special precaution: ECG should be recorded 1 & 3 week/s after treatment. Patients with
prostatic hypertrophy, glaucoma, renal dysfunction, pre-existing
convulsive disorders, patient with cardiac pacemakers, limited renal
function, and organic brain syndrome.
Contraindications: Narrow angle glaucoma. Because of its atropine like side effects,
this drug is contraindicated in children less than 3 years of age, and
should be used with caution in older children.
Pregnancy: The safe use of this drug in pregnancy has not been established.
Cardiovascular: Tachycardia.
Dosage:
Benztropine mesylate should be used orally in all cases when patients are able to take
oral medication. In other cases, where more rapid response is desired, benztropine
mesylate may be administered i.v. or i.m.
Since there is no significant difference in onset of effect after i.v. and i.m. injection,
usually there is no need to give benztropine i.v. It is quickly effective after either route,
with improvement sometimes noticeable a few minutes after injection. In emergency
situations, 1 to 2 mg of benztropine mesylate parenterally normally will provide quick
relief. If the parkinsonian effect begins to return, the dose can be repeated.
Because benztropine has cumulative action, therapy should be initiated with a low dose
which is increased gradually at 5 or 6 day intervals to the smallest amount necessary for
optimal relief. The initial dose should be 0.5 mg daily. Increases should be made in
increments of 0.5 mg to a maximum of 6 mg or until optimal results are obtained without
excessive adverse effects.
Therapy with other agents should not be terminated abruptly when therapy with
benztropine mesylate is initiated, but may be reduced or discontinued gradually.
Benztropine mesylate may be administered concomitantly with levodopa or a
levodopa/carbidopa combination, in which case the dose of each may need adjustment.
Benztropine mesylate should not be used beyond the period necessary to counteract the
extrapyramidal manifestations. Although medication with the drug causing parkinsonism
can frequently be continued without change of dosage when adjunctive therapy with
benztropine is used, a reduction in dosage of the psychotropic drug might be indicated.
Patients must be closely observed for severe reactions and benztropine mesylate
discontinued temporarily if they appear.
AKINETON Abbott
[Zuellig]
Contents: Biperiden
Diazepam
Brand name: T-Quil, Valium
Diazepam is relatively devoid of autonomic effects and does not significantly reduce
locomotor activity at low doses, or depress amphetamine-induced excitation. In high
doses, it activates the drug metabolizing enzymes in the liver. Diazepam also possesses
dependence liability and may produce withdrawal symptoms, but has a wide margin of
safety against poisoning.
Metabolism studies in animals and man have indicated that oral diazepam is rapidly
absorbed from the gastrointestinal tract. Peak blood levels are reached within 1-2 hours
after administration. The acute half-life is 6-8 hours with a slower decline thereafter,
possibly due to tissue storage.
In humans, comparable blood levels of diazepam were obtained in maternal and cord
blood indicating placental transfer of the drug. Diazepam may appear in human breast
milk.
With the parenteral form, peak blood levels are reached within 15 minutes after i.v.
administration and are of the same magnitude as after oral administration. The
respective half-life is approximately 2-3 hours.
The distribution and fate of tritium-labeled diazepam in man has indicated that the drug
has a rapid and extensive uptake by tissues. Although the radioactivity in the blood
appears to represent mainly the intact drug, diazepam was shown to be excreted
exclusively in the form of its metabolites. The two major metabolites are oxazepam
glucuronide and N-desmethylated diazepam.
Precautions:
Geriatrics:
Elderly and debilitated patients or those with organic brain disorders have been found to
be prone to CNS depression following even low doses. For these patients it is
recommended that the dosage be limited to the smallest effective amount to preclude
development of ataxia, oversedation or other possible adverse effects.
Drug dependence:
Abrupt cessation of large doses of diazepam after prolonged periods may precipitate
acute withdrawal symptoms and, in these cases, the drug should be discontinued
gradually. Caution should be exercised when it is considered necessary to administer
diazepam to addiction prone individuals.
Adverse Effects: The most common adverse effects reported are drowsiness and
ataxia. Other reactions noted less frequently are fatigue, dizziness,
nausea, blurred vision, diplopia, vertigo, headache, slurred speech,
tremors, hypoactivity, dysarthria, euphoria, impairment of memory,
confusion, depression, incontinence or urinary retention,
constipation, skin rash, generalized exfoliative dermatitis,
hypotension, changes in libido.
The more serious adverse reactions occasionally reported are
leukopenia, jaundice, hypersensitivity and paradoxical reactions.
Dosage:
Adults:
Symptomatic relief of anxiety and tension in psychoneurosis and anxiety reactions: 2 to
10 mg, 2 to 4 times daily depending upon severity of symptoms.
Symptomatic relief in acute alcohol withdrawal: 10 mg, 3 or 4 times during the first 24
hours, reducing to 5 mg, 3 or 4 times daily as needed.
Children (Because of varied responses, initiate therapy with lowest dose and increase as
required. Not for use in children under 6 months):
1 to 2.5 mg, 3 or 4 times daily initially; increase gradually as needed and tolerated.
Drug classes: Benzodiazepine, Anxiolytic, Sedative-hypnotic
Therapeutic actions:
Exact mechanisms are not understood; acts mainly at subcortical levels of the CNS,
leaving the cortex relatively unaffected. Main sites of action may be the limbic system
and reticular formation; benzodiazepines potentiate the effects of GABA, an inhibitory
neurotransmitter; anxiolytic effects occur at doses well below those needed to cause
sedation and ataxia.
Indications:
Available forms:
Oral
Usual dose is 2–6 mg/day; range 1–10 mg/day given in divided doses with largest
dose hs.
IM
IV
Initial dose is 2 mg total or 0.044 mg/kg, whichever is smaller. Do not exceed this dose in
patients older than 50 yr. Doses as high as 0.05 mg/kg up to a total of 4 mg may be given
15–20 min before the procedure to those benefited by a greater lack of recall. Continuous
infusion 0.5–1 mg/hr titrated, based on patient response.
PEDIATRIC PATIENTS
Pharmacokinetics
IV facts
Adverse effects
Pharmacology:
Antiparkinsonian
Pharmacokinetics:
Trihexyphenidyl is rapidly absorbed from the gastrointestinal tract. After oral
administration, the onset of action occurs within 1 hour, peak effects last 2 to 3 hours
and the duration of action is 6 to 12 hours. It is excreted in the urine, probably as
unchanged drug.
Indications
Closely observe patients with cardiac, liver, kidney or hypertensive disorders. Patients
undergoing prolonged therapy should be subjected to careful periodic review to avoid
untoward reactions. Trihexyphenidyl should be used with caution in patients with
glaucoma, obstructive disease of the gastrointestinal or genitourinary tracts, and in
elderly males with possible prostatic hypertrophy. Trihexyphenidyl may cause
anhidrosis. Caution should be exercised during hot weather especially if given with other
anticholinergic drugs. Incipient glaucoma may be precipitated by trihexyphenidyl.
Geriatrics:
Geriatric patients, particularly over the age of 60, frequently develop increased sensitivity
to parasympatholytic drugs and hence, require strict dosage regulation.
Adverse Effects
Potential untoward effects associated with the use of any atropine like drugs include
constipation, drowsiness, urinary hesitancy or retention, tachycardia, postural
hypotension, dilatation of the pupil, increased intraocular tension, weakness, vomiting,
and headache.
Dosage
Should be individualized. The initial dosage should be low and then increased gradually,
especially in patients over 60 years of age.
Parkinsonism:
1 mg orally the first day; increased by 2 mg daily at intervals of 3 to 5 days, up to 6 to 10
mg daily. Best tolerated in divided dose at mealtime.
Drug-induced Parkinsonism:
The size and frequency of doses of trihexyphenidyl needed to control drug induced
extrapyramidal reactions, attributable especially to reserpine and phenothiazine
derivatives, must be determined empirically. The total daily dosage usually ranges
between 5 and 15 mg although, in some cases, these reactions have been satisfactorily
controlled on a little as 1 mg daily. It may be advisable to commence therapy with a
single 1 mg dose. If the extrapyramidal manifestations are not controlled in a few hours,
the subsequent doses may be progressively increased until satisfactory control is
achieved. Satisfactory control may sometimes be more rapidly achieved by temporarily
reducing the dosage of the antipsychotic or instituting trihexyphenidyl therapy and then
adjusting dosage of both drugs until the desired antipsychotic effect is retained without
onset of the extrapyramidal reactions.