Mode of action: it slows down the reuptake of
5-hydroxytryptamine and norepinephrine, to a small extent –
dopamine. Mode of action stipulates an ability of the medicine to
enhance the transmission of nerve impulses into the central nervous
Venlafaxine absorbs and metabolizes
well after the ingestion in the liver. Meal does not influence much
on absorption and biotransformation of venlafaxine.
It takes out from the organism with the help of the gemmae.
Treat for depression with attending anxiety, secondary prophylaxis
and depressive disorder (in hospital or in the community setting).
There are the groups of side effects that depend on frequency
of emergence: frequent – more than 1%, infrequent - 0.1-1%, seldom -
0.01-0.1%, very seldom – less than 0.01%.
Nervous system: frequent - headache,
insomnia, nightmares, nervosism, paresthesia, muscle hypertonia,
tremor, sedation; infrequent - apathy, hallucinations, myoclonus,
faintness; seldom - spasms, mania, neuroleptic malignant syndrome.
CVS: frequent - elevation of arterial
tension, hyperemia of skin integument; infrequent - drop
of arterial tension, postural hypotension, tachycardia.
Digestive system: frequent -
reduction of appetite, sickness, vomiting, infrequent - bruxism
(unintentional teeth-grinding), hepatic transaminitis;
seldom - hepatitis.
Urogenital system: frequent -
decreased interest, erection disorder and/or ejaculation disorder ,
anorgasmia, menorrhagia, acraturesis; infrequent - uroschesis, women
Sensory organs: frequent -
accommodation disorder, mydriasis, vision impairment; infrequent -
taste perception disorder.
Hemopoietic system (for capsule):
frequency unknown - agranulocytosis,
anaemia, hypogranulocytosis, pancytopenia.
Hypersensitivity reaction: infrequent
- eruption, photosensitization; anaphylactic reaction.
Lab values: infrequent -
thrombocytopenia; seldom – rising bleeding time,
hyponatremia; by long-term use of high doses - hypercholesterinemia.
Others: frequent - body weight loss,
hyperspiration (including at night); infrequent - ecchymosis, body
weight gain; seldom - syndrome of inappropriate secretion of
antidiuretic hormone (SIADH), when intake capsules - serotonin
syndrome (sickness, vomiting, abdominal pains, diarrhea, meteorism,
psychomotor agitation, tachycardia, hyperthermia, muscular rigidity,
spasms, myoclonus, hyperhidrosis, impairment of
consciousness from delirium to semicoma and coma with fatality).
With the origin of withdrawal state:
dizziness, headache, asthenia, tirednesssleep disturbance (changing
the type of dreams, sleepiness or insomnia, sleep-onset insomnia),
anxiety, nervosism, mental confusion, paresthesia, hyperhidrosis, xerostomia, reduction of appetite, sickness, vomiting, diarrhea
(majority of these reactions represent insignificantly and do not
need to be cure).
Hypersensibility, polypharmacy with
inhibitors of monoamine oxidase, pregnancy, service period, under
18 years of age. With precaution. Recently old myocardial
infarction, unstable angina, arterial hypertension, tachycardia,
spasms in anamnesis, ocular hypertension, narrow-angle glaucoma,
mania in anamnesis, hyponatremia,
simultaneous dose of diuretics, suicidal tendencies, predisposition
to bleeding from the part of skin and mucous membrane, nephatony
The prescription of venlafaxine
is possibly only not until 14 days
from the moment of treatment cessation with inhibitors of monoamine
oxidase and has to be stopped not less than 7 days before the
beginning of taking any inhibitor of monoamine oxidase (possibly
development or increase of giddiness, sickness, vomiting,
hyperperspiration, hyperemia of skin, tremor, myoclonia,
hyperthermia, signs, that are similar to neuroleptic malignant
syndrome, spasms, up to fatal outcome).
During curing you should control
blood pressure. Remember that at the beginning of curing you can
have the desire to commit a
suicide. For decrease the probability of overdosage it is important
to give the patient minimum of the drug at the beginning of curing.
Hyponatremia and/or syndrome of
inappropriate secretion of antidiuretic hormone could be developed
during treatment at the patients associated with oligemia or dried
(including elderly patients, who taking diuretics).
The bleeding of skin and mucous
membrane can be increased during curing with venlafaxine that
is why it is necessary to be very careful when it is used by
patients with predisposition to bleeding.
If venlafaxine has been used
directly before labor or shortly before childbirth,
it is important to take into account the possibility of development
of withdrawal state at a newborn.
The medicine practically does not
influence on the speed of healthy volunteers’ psychomotor actions,
their cognition and mixed behavioral response. Nevertheless, taking
into consideration the possibility of appearance significant side
effects from the part of CNS, during treatment it is necessary to be
careful when driving a car and doing potential dangerous kind of
activity, those require heightened attention focusing and quickness
of psychomotor actions.
It is recommended not to take ethanol
raises anticoagulant impact of warfarin.
It enhances influence of ethanol on
Cinamet restrains metabolism of the
venlafaxine’s first undergoing and
does not influence on pharmacokinetics.
It increases AUC risperidone 32%, but
does not influence essential on total disposition profile of active
Does not integrate with preparations
that including lithium.
Intake with food. It is advisable to take it at the regular hours,
not chewing and taking some water with it.
Pills: recommended beginning dose is
37.5 mg twice a day.
If warranted the dosage interval can be increased not less than 4
days at 75
Recommended dose if you have moderate depression is 225 mg per day
at 3 stages, if you have hard depression -
maximum permissible daily dose is 375
mg at 3 stages.
Capsules (do not divide, do not
powder and do not dissolve in water): recommended beginning dose is
75 mg once per day; if warranted the dosage interval can be
increased not less than 4 days up to 2 weeks and more. Maximum daily
dose is 225 mg.
The patients, who has been getting
pills, can be transferred to take capsules at the similar doses.
Gradual withdrawal will help to avoid
withdrawal state: if the course of treatment consists of 6 weeks and
more the period gradual withdrawal of the medicine should have not
less than 2 weeks and depends on dosage, duration of therapy and
patient’s individual peculiarities (in clinical testing of capsules
the dose was reduced by 75 mg once per week).
With renal disorder (the speed of
glomerular filtration is 10-70 ml/min) the daily dose has to be
reduced by 25-50%.
With hemodialysis the daily dose has
to be reduced by 50%, you should take the medicine after ending the
treatment of hemodialysis.
The daily dose of patients with
moderate hypohepatia has to be reduced by 50% and
Escilopram (Lexapro)Antidepressant, the mechanism of action is based
on selective serotonin
is linear and depends
on the dose
the range of
10–30 mg daily. The maximum concentration in the blood plasma is
attained during 5 hours after taking the medicine inside.
absorption does not depend on the simultaneous meal. Bioavailability
about 80%. The volume
12 l/kg of
Approximately 56% of escitalopram
chemically bound with blood plasma proteins.
When taking once daily the equilibrium state is achieved in average
in 1 week.
generalized anxiety disorder.
biotransformation is principally done inside the
do not have an important
is 27–32 h.
excreted in the urine, about
8% in the form of escitalopram
and 10% — in the form of S-demetiltsitalopram.
The starting dose is 10 mg once daily. The
dose may be increased to 20 mg once daily after 1 week.
It is taken once daily (in the morning or evening), with or without
food. The dose for patients having a
hepatic failure and patients of advanced age
should not be over 10 mg/daily.
dose correction is not necessary for
In case of
major depressive disorder
maintenance therapy is carried out in the dose of
10–20 mg daily during several months (taking
into account the clinical situation).
The duration of treatment in case of
generalized anxiety disorder is ordinary up to 8 weeks.
simultaneous use of Mao inhibitors.
common side effects associated with escitalopram are
ejaculatory delay, difficulty sleeping or
Generally escitalopram does not have negative effect on the
you should avoid driving transport vehicles and working with
potentially dangerous mechanisms before finding
individual reaction on the treatment.
Prescription of the drug in the period of pregnancy is possible only
if the expected
effect for the mother
exceeds potential risk for the fetus.
effects of alcohol
on the central nervous system, however alcohol is not recommended
While using the drugs with
acetylsalicylic acid, other non-steroidal, anti-inflammatory and
other grugs with
effect, the risk of development of gastro-intestinal
While using selective serotonin reuptake inhibitors with
isolated cases of weakness, hyperreflexia and discoordination are
in case of such kind of treatment the patient has to be
combined use with ketoconazole may occur a reduced concentration
in the blood plasma.
Cases of overdose with escitalopram’s
treatment at the dose to
600 mg are discribed; any symptoms of the
intoxication were not observed. The overdose of
in the dose of 2 g did not lead to death. The lethal outcome is
possible is case of a more important overdose, mainly when combined
psychotropic drugs or alcohol.
The main complications caused by escitalopram’s
Amnesia, mental confusion, koma, hyperventilation, cyanosis,
rhabdomyolysis, cardiogram changes are rarely observed.
order to maintain an adequate ventilation and
oxygenation it is necessary to provide the patency
the upper respiratory tract, control B.P., ECG and the external
There is no specific antidote; the treatment is supporting and
symptomatic. Because of a big volume of escitalopram’s
dialysis, hemoperfusion and exchange blood transfusion have little