Chlorphenamine(chlorpheniramine)

Chlorphenamine
Pharmaceutical Form
Clear, colorless sterile solution for
injection.
Chlorphenamine injection is indicated for
acute urticaria, control of allergic
reactions to insect bites and stings,
angioneurotic oedema, drug and serum
reactions, desensitisation reactions,
hayfever, vasomotor rhinitis, severe
pruritus of non-specific origin.
Systematic (IUPAC) name
Posology And Method Of Administration:
Adults:
3-(4-chlorophenyl)-N,N-dimethyl-
The usual dose of chlorphenamine
3-pyridin-2-yl-propan-1-amine injection for adults is 10mg to 20mg, but
not more than 40mg should be given
within a 24-hour period. The injection
may be given by the subcutaneous, intramuscular
or intravenous route.
Synonyms】
2-(p-Chloro-alpha-(2-
Age Dose (dimethylamino)ethyl)benzyl)pyridine
maleate (1:1)
1 month 0.25mg/kg Product Name】
to 1 year Chlorphenamine hydrogen maleate
【Formula】
C20H23ClN2O4
Molecular Weight】
1 to 5 2.5mg to 5mg OR 0.20mg/kg 390.9
years
Appearance
Odorless white crystalline solid or
6 to 12 5mg to 10mg OR 0.20mg/kg white powder with a bitter taste.
years Melting Point】
131 – 133
Chlorphenamine Point de fusion
12 to 18 10mg to 20mg OR 0.20mg/kg 142 oC (boiling point)
years
Solubility in water
0.55 g/100 mL, liquid mg/mL (20 °C)

• Chlorpheniramine is an antihistamine that helps to relieve allergic disorders due

to cold, hay fever, itchy skin, insect bites and stings.
 Chlorpromazine

Systematic (IUPAC) name

3-(2-chloro-10H-phenothiazin-10-yl)-N,N-dimethyl-propan-1-amine

Formula: C17H19ClN2S

Adverse effects

The main side effects of chlorpromazine are due to

its anticholinergic properties; these effects overshadow and counteract, to some extent,
the extrapyramidal side effects typical of many early generation antipsychotics. These
include sedation, slurred speech, dry mouth, constipation, urinary retention and possible
lowering of seizure threshold. Appetite may be increased with resultant weight gain, and
Glucose tolerance may be impaired.[21] It lowers blood pressure with accompanying
dizziness.[14] Chlorpromazine, which has sedating effects, will increase sleep time when
given at high doses or when first administered, although tolerance usually develops.[22]
Sleep cycles or REM sleep is not altered by antipsychotics.[23]

Dermatological reactions are frequently observed. In fact three types of skin disorders are
observed: hypersensitivity reaction, contact dermatitis, and photosensitivity. During long-
term therapy in schizophrenic patients chlorpromazine can induce abnormal pigmentation
of the skin. This can be manifested as gray-blue pigmentation in regions exposed to
sunlight.[22]

There are adverse effects on the reproductive system. Phenothiazines are known to cause
hyperprolactinaemia leading to amenorrhea, cessation of normal cyclic ovarian function,
loss of libido, occasional hirsutism, false positive pregnancy tests, and long-term risk of
osteoporosis in women. The effects of hyperprolactinemia in men are gynaecomastia,
lactation, impotence, loss of libido, and hypospermatogenesis. These antipsychotics have
significant effects on gonadal hormones including significantly lower levels of estradiol
and progesterone in women whereas men display significantly lower levels of
testosterone and DHEA when undergoing antipsychotic drug treatment compared to
controls.[24] According to one study of the effects on the reproductive system in rats
treated with chlorpromazine there were significant decreases in the weight of the testis,
epididymis, seminal vesicles, and prostate gland. This was accompanied by a decline in
sperm motility, sperm counts, viability, and serum levels of testosterone in
chlorpromazine rats compared to control rats. It has been reported that a change in either
the absolute or relative weight of an organ after a chemical is administered is an
indication of the toxic effect of the chemical. Therefore, the observed change in the
relative weight of the testis and other accessory reproductive organs in rats treated with
chlorpromazine indicates that the drug might be toxic to these organs at least during the
period of treatments. Furthermore, the weights of the kidney, heart, liver, and adrenal
glands of these treated rats were not affected both during administration of the drug and
recovery periods, suggesting that the drug is not toxic to these organs.[24]

Antipsychotic drugs may cause priapism, a pathologically prolonged and painful penile
erection, which is usually unassociated with sexual desire or intercourse. Although this
effect is rare it is a potentially serious complication that can lead to permanent impotence
and other serious complications.[25]

Even therapeutically low doses may trigger seizures in susceptible patients, such as those
with an abnormally low genetically determined seizure threshold, presumably by
lowering the seizure threshold. The incidence of the first unprovoked seizure in the
general population is from 0.07 to 0.09%, but in patients treated with commonly used
antipsychotic drugs it reportedly ranges from 0.1 to 1.5%. In overdose, the risk reaches 4
to 30%. This wide variability among studies may be due to methodological differences.
The risk is greatly influenced by the individual's inherited seizure threshold, and
particularly by a history of epilepsy, brain damage or other conditions. The triggering of
seizures by antipsychotic drugs is generally agreed to be a dose-dependent adverse effect.
[26]

Tardive dyskinesia and akathisia are less commonly seen with chlorpromazine than they
are with high potency typical antipsychotics such as haloperidol[27] or trifluoperazine, and
some evidence suggests that, in conservative dosing, the incidence of such effects with
chlorpromazine may be comparable with that of newer agents such as risperidone or
olanzapine.[28]

A particularly severe side effect is neuroleptic malignant syndrome, which can be fatal.[29]
Other reported side effects are rare, though severe; these include a reduction in the
number of white blood cells—referred to as leukopenia—or, in extreme cases, even
agranulocytosis, which may occur in 0.01% of patients and lead to death via
uncontrollable infections and/or sepsis. Chlorpromazine is also known to accumulate in
the eye—in the posterior corneal stroma, lens, and uveal tract. Because it is a phototoxic
compound, the potential exists for it to cause cellular damage after light exposure.
Research confirms a significant risk of blindness from continued use of chlorpromazine,
as well as other optological defects such as color blindness and benign pigmentation of
the cornea.[30]

Cardiotoxic effects of phenothiazines in overdose are similar to that of the tricyclic

antidepressants.[22] Cardiac arrhythmia and apparent sudden death have been associated
with therapeutic doses of chlorpromazine, however they are rare cases. The sudden
cardiovascular collapse is attributable to ventricular dysrhythmia. Supraventricular
tachycardia may also develop. Patients on chlorpromazine therapy exhibit abnormalities
on the electrocardiographic T and U waves. These major cardiac arrhythmias that are
lethal are a potential hazard even in patients without heart disease who are receiving
therapeutic doses of antipsychotic drugs. In order to quantify the risk of cardiac
complications to patients receiving therapeutic doses of phenothiazines a prospective
clinical trial is suggested.[31]