(and dosage form):
Slow Release Capsule
Each capsules contains Lithium Carbonate Microcaps, 400 mg.
A 1.2. Central Nervous system stimulants. Psycho-analeptics (antidepressants).
The specific biochemical mechanism of lithium action is unknown. Lithium alters sodium transport in nerve and muscle cells and effects a shift towards intraneuronal metabolism of catecholamines.
Acute mania and manic states involving mild levels of hyperactivity and excitation; it may also be effective in certain patients with depression, but the chance of success cannot be predicted.
Impaired renal function, cardiac disease, evidence of brain damage and in patients on a salt-free diet.
DOSAGE AND DIRECTIONS FOR USE:
0,4 - 1,2 g as a single daily dose taken early in the morning. Such a dosage will normally produce a serum lithium level ranging between 0,5 - 0,1 mEq/L.
Maintenance: Desirable blood levels are 0,5 - 1,0 mEq/L.
In acute mania high doses of lithium are often needed to achieve therapeutic effect. It is important, however, that the dosage be reduced rapidly to maintenance levels when the acute attack subsides.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Lithium toxicity is closely related to serum lithium levels, and can occur at doses close to therapeutic levels. Facilities for prompt and accurate serum lithium determinations should be available before initiating therapy. Adverse reactions are seldom encountered at serum lithium levels below 1,5 mEq/L except in the occasional patients usually sensitive to lithium. Mild to moderate toxic reactions may occur at levels from 1,5 to 2,5 mEq/L and moderate to severe reactions may be seen at levels from 2,0 to 2,5 mEq/L, depending upon the individual response to the drug.
Patients on the therapeutic doses of lithium may complain of fatigue and muscular weakness.
Fine hand tremor, slurred speech, polyuria and mild thirst may occur during initial therapy for the acute manic phase, and may persist throughout treatment. Transient and mild nausea and general discomfort may also appear during the first few days of lithium administration. Toxic signs are rarely seen in patients stabilized on maintenance doses.
Diarrhoea, vomiting, drowsiness, muscular weakness and lack of co-ordination may be early signs of lithium intoxication, and can occur at lithium levels below 2,0 mEq/L. At higher levels, ataxia, giddiness, tinnitus, blurred vision, and a large output of dilute urine may be seen.
Serum lithium levels above 3,0 mEq/L may produce a complex clinical picture, involving multiple organs and organ systems. Serum lithium levels should not be permitted to exceed 2,0 mEq/L during the acute treatment phase, or 1,5 mEq/L during maintenance therapy.
The following toxic reactions have been reported and appear to be related to serum lithium levels.
Neuromuscular: tremor, muscle hyperirritability (fasciculations, twitching, clonic movements and hyperextension of whole limbs), ataxia, choreo-athetotic movements, muscular rigidity, hyperactive deep tendon reflex.
Central Nervous System: blackout spells, epileptiform seizures, slurred speech, dizziness, vertigo, muscular rigidity, incontinence of urine and faeces, somnolence, psychomotor retardation, restlessness, and cranial nerve and focal neurological signs progressing to confusion, stupor, coma and death.
Cardiovascular: cardiac arrhythmia, hypotension, peripheral circulatory collapse.
Gastrointestinal: anorexia, nausea, vomiting, diarrhoea, dry mouth.
Genito-urinary: albuminuria, oliguria, polyuria, glycosuria.
Allergic: allergic vasculitis.
Dermatologic: drying and thinning of hair, anaesthesia of skin.
Autonomic: blurred vision.
Miscellaneous: fatigue, lethargy, transient scotomata, dehydration, weight loss.
Acquired nephrogenic diabetes insipidus accompanied by excessive thirst is frequently seen.
Exophthalmos has been reported. Leucocytosis occurs in many patients.
Adverse reactions apparently unrelated to dosage include;
Thyroid toxicity: (goitre formation, lowering of P.B.I., increased I131 uptake);
E.E.G. Changes: (diffuse slowing, widening of the frequency spectrum, potentiation and disorganisation of background rhythm);
E.C.G. Changes: (reversible flatttening, iso-electricity or inversion of T waves).
Miscellaneous: thirst, leg ulcers, headache, transient hyperglycemia, generalised pruritus with or without rash, swelling of ankles or wrist and metallic taste.
While most side-effects are more common during the first week or two of treatment and usually disappear when the dose is reduced, thirst, excessive urination and tremor may persist.
The ability to tolerate lithium is considerably increased during the acute manic phase and decreases markedly when manic symptoms subside.
The distribution space of lithium approximates that of total body water. Lithium is primarily excreted in urine, with insignificant excretion in faeces. Renal clearance of lithium is proportional to its plasma concentration. Lithium decreases sodium reabsorption by the renal tubules which could lead to sodium depletion. Therefore, it is essential for the patients to maintain a normal diet, including salt, and an adequate fluid intake (2 500 - 3 000 mL) at least during the initial stabilization period.
When sodium intake is lowered, lithium excretion is slower and severe intoxication may ensure. Thus, lithium should not be given to patients on a salt-free diet. In pregnancy, concomitant use of natiuretics (diuretics) and low-sodium diets is the most common cause of maternal and neonatal lithium intoxication. Decreased tolerance to lithium has been reported to ensue from protracted sweating or diarrhoea and if such occur, supplemental fluid and salt should be administered. Diuretics should not be used concomitantly with lithium carbonate therapy.
The physician should be alert for possible thyroid involvement. Diffuse non-toxic goitre has been reported in a small number of patients on maintenance therapy with lithium and in one baby born to a lithium-treated mother.
KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Coma with hyper-reflexia, muscle tremor, attacks of hyper-extension of the limbs, and occasionally epileptic seizures.
Early symptoms of toxicity can usually treated by reduction of dosage or withdrawal of the drug. In severe cases of toxicity, gastric suction and replacement of fluids and electrolytes have been suggested. Sodium bicarbonate, acetazolamide and aminophylline produce significant increase of lithium excretion.
CONDITION OF REGISTRATION:
To be advertised only to the medical profession.
Green and yellow capsules.
100 capsules per securitainer.
Store in cool (below 25°C), dry place.
KEEP OUT OF REACH OF CHILDREN.
NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Adcock Ingram Park
17 Harrison Ave
Bryanston Ext. 77
Private Bag X69, Bryanston, 2021
DATE OF PUBLICATION OF THIS PACKAGE INSERT:
21 November 1978
New addition to this site: April 2004
Source: Pharmaceutical Industry
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