Central Nervous System
Depressants
ANTIPSYCHOTIC
AGENTS
“Typical”
–
derivatives
of
phenotiazine,
tioxanten,
butyrophenon – they cause
disorders
of
extrapyramidal
system function – syndrome of
parkinsonism
“Atypical” – derivatives of indole,
benzodiazepine – they cause those
negative reactions very rarely
Aminazine (chlorpromazine)
• 1951 – aminazine was introduced into clinical
practice
• It brought considerable changes into situations
of psychiatric clinics
• Before appearance of aminazine for treatment of
psychologically sick patients insulin or electric
shock were widely used, in some cases lobotomy
Phenothiazine derivatives
Thioxanten derivateves
Butyrophenon derivatives
piperasine-dibenzodiazepine derivatives
(Clozapin, Clozapine, FazaClo, Leponex, Zaponex, Clopin
Eco.)
Mechanism of action of
neuroleptics
Influence on dopamine (D2), noradrenergic,
serotoninergic, GABA-ergic, cholinergic
receptors
Properties of neuroleptics
• Antipsychotic action - they eliminate
productive symptoms of psychosis
(delirium and hallucinations), affective
disorders
• They eliminate psychomotor excitation
• consciousness is present
1 Lung Cancer, 2 Criminality, 3 Stroke, 4 Breast Cancer, 5 Same Sex
Attraction, 6 Leukemia, 7 Malformation, 8 Alzheimer’s, 9 Ulcerative
Colitis, 10 Rheumatoid Arthritis, 11 Alcoholism,
12 Schizophrenia, 13 Depression, 14 Suicide attempt,
15 Diabetes type I, 16 Divorce, 17 Crohn’s disease, 18 Asthma, 19
Hypertension, 20 Co twin is best friend, 21 Diabetes type II, 22 Autism,
23 Opposite Sex Attraction, 24 Phenylketonuria
Administration of antipsychotic action
of neuroleptics
Treatment of psychosis
•
•
•
•
Schizophrenia
Maniac-depressive psychosis
Alcohol psychosis
Reactive psychosis
In a case of psychomotor excitation
of various etiology
Delirium tremens –
alcohol psychosis
Influence of neuroleptics on psychical
activity
1. Drugs with psychosedative action – they cause
condition of psychomotor indifference (apathy, decreasing
of moving activity, retarded emotions and wishes,
disappearance of initiative)
Aminazine, clozapine (leponex), chlorprotyxen,
haloperidol, droperidol
Peculiarities of usage: psychosis with manifestations of
excitation
Contraindications: psychosis with retardness, inertia,
depression, stupor, apatho-abulic syndrome
Neuroleptics with psychosedative action
Influence of neuroleptics on psychical
activity
2. Drugs which stimulate psychical activity
(increase mimics and liveliness, increase moving
activity, improve the mood)
Triftazin, ethaperazin, moditen, majeptil
Peculiarities of usage:
psychosis with psychomotor retardness, apathoabulic conditions, stupor conditions
Contraindications: affective disturbances,
mania, psychomotor excitation
Drugs which stimulate psychical
activity
Other properties and indications for
administration of neuroleptics
• Drugs with psychosedative action – for potentiation of action of
hypnotic drugs, opioid and nonopioid analgesics, drugs for general
anesthesia, local anesthetics, for example, neuroleptanalgesia
• Anti-emetic action (elimination of vomiting of central origin):
brain tumors, radial and chemical therapy, intestinal impassability,
intoxication with heart glycosides, apomorphine and other drugs
• Decreasing of body temperature (only in the case of simultaneous
hypothermia)
• Decreasing of blood pressure (alpha-adrenoblocking properties –
aminazine, droperidol) – in case of hypertensive crisis, lungs, brain
edema
Side effects of neuroleptics
• Extrapyramidal disorders: muscular hypertonus, general
constraint, tremor of hands, tongue, mandible, head, seizure
contractions of muscles, vegetative crisis
For treatment – cyclodol (levodopa is contraindicated because it
diminishes therapeutic effect of neuroleptics)
• Orthostatic collapse
• Complicated nose breathing, hypostatic, aspirate pneumonia
• Dyspeptic disorders: anorexia, changes of taste
• Abdominal pain
• Constipation
• Damage of the liver (cholestasis)
• Granulocytopenia (especially clozapin)
• Hyperglycemia, dysmenorrhea, galactorrhea, hyperthyrosis,
gynecomastia, impotence
• Aminazine has a considerable irritative action
syndrome of parkinsonism
Parkinsone syndrome treatment
Cyclodolum
Levodopa is
contraindicated
TRANQUILIZERS
• Agonists of benzodiazepine receptors:
- derivatives of benzodiazepine – chlozepid,
sybazon, phenazepam, gidazepam
• Agonists of serotonine receptors: buspyrone
• Drugs with other mechanisms of action:
- derivatives of diphenilmethan: amisyl
- derivatives of propanediole: meprotan
TRANQUILIZERS
Properties of tranquilizers
• Anxiolytic properties – eliminate feeling of
anxiety, restlessness, fear, aggressiveness,
irritability, cause peace, careness, decreasing of
moving activity
• Hypnotic (somnolent) action
• Myorelaxing action (of central genesis)
• Antiseizure action
Administration of tranquilizers
Anxiolytic action
• Treatment of neurosis, accompanied by fear, anxiety,
exertion, increased irritability, insomnia
• In case of headache and heart pain of neurotic origin,
so called organic neurosis
• In case of abstinence in alcohol and drugs addicts
• In case of diencephalons crisis (sybazon)
Tranquilizers do not diminish productive symptoms
of psychosis!
Administration of tranquilizers
Anti-seizure and myorelaxing action
(depression of CNS structures, braking polysynaptic spinal
reflexes)
sybazon, fenazepam
• In a case of seizures of any etiology (epileptic status,
tetanus, poisoning with seizure causing poisons) sibazon
is introduced intravenously (intramuscularly) – 2-4 ml
of 0,5 % solution repeatedly (maximum daily dose – 14
ml)
• To eliminate muscle tension in a case of radiculitis,
arthritis, myositis, bursitis
Seizures
(tetanus)
drug of a first choice -
Sibazon
SIDE EFFECT OF TRANQUILIZERS
•
Psychological and physical addiction
Prophylaxis:
1.
Duration of treatment course should not be more than 2 months
2.
Repeated course – not earlier than after 3 weeks break
•
Sleepiness, reeling walk, retarded reactions
tranquilizers should not be administered in ambulatories to people whose
professions are connected with quick reactions
•
Paradox reaction of excitation, insomnia
• Dizziness, decreasing of libido, disturbances of
menstrual cycle
• Uncontrolled urination, defecation, ataxia,
dysarthria
• Acute poisoning in case of overdosing
FLUMAZENIL (ANEXAT)
ANTAGONIST OF TRANQUILIZERS
Combination of
tranquilizers with
alcohol-containing
drinks is absolutely
contraindicated
(pathological alcohol
intoxication)
Valeriana
PASSIFLORA
Leonurus L.
dog nettle
ADMINISTRATION OF
SEDATIVE DRUGS
•
•
•
•
•
•
Neurosis
Neurasthenia
Hysteria
Increased irritability
Insomnia
Primary stages of essential hypertension
Bromism
• Cause – accumulation of bromide ions in organism
in case of their prolonged administration as a result
of material accumulation
• Symptoms: rhinitis, cough, conjunctivitis, skin
rash, general weakness, memory disorders
• Treatment: sodium chloride (10-20 g / day), a lot of
drinking (3-5 l / day), regular and frequent cleaning
of skin and digestive tract
Hypnotic agents
CNS Depressants
Hypnotics
• Calm or soothe the CNS to the point that
they
cause sleep
Sedative-Hypnotics—dose dependent:
• At low doses, calm or soothe the CNS
without inducing sleep
• At high doses, calm or soothe the CNS
• to the point of causing sleep
Epilepsy
• In the U.S., 2.5
million people
are affected.
• Not all seizure
disorders are
epilepsy.
Epilepsy
Seizure
Abnormal electrical discharges in the cerebral cortex
caused by sudden, excessive firing of neurons
– Result in a change in behavior of which the patient is
not aware
– While conscious, the patient may or may not lose
movement control
– Loss of body control may affect one area or the entire
body
Drug List
Anticonvulsants
•
•
•
•
•
•
•
•
•
•
lamotrigine (Lamictal)
levetiracetam (Keppra)
lorazepam (Ativan)
oxcarbazepine (Trileptal)
phenobarbital (Luminal Sodium)
phenytoin (Dilantin)
primidone (Mysoline)
topiramate (Topamax)
valproic acid (Depakene)
zonisamide (Zonegran)
• carbamazepine (Epitol,
Tegretol)
• clonazepam (Klonopin)
• diazepam (Valium)
• divalproex (Depakote)
• ethosuximide (Zarontin)
• Fosphyenytoin (Cerebyx)
• gabapentin (Neurontin)
valproic acid (Depakene) and
divalproex (Depakote)
• Increases the availability of GABA
(inhibitory)
• Take with water, not a carbonated drink
• Do not use aspirin
Dispensing Issues
Warning!
• Depakote and Depakene can easily be
confused.
• Be careful with Depakote and Depakote ER.
• Depakote ER is only once a day.
Parkinson’s Disease
Physiology
• Normal muscle movement requires balance of
dopamine (inhibitor) and ACh (stimulator)
• In the substantia nigra, enough dopamine is
released to counteract the effects of ACh
• In parkinsonism, enough dopamine is not released
which leads to excessive motor nerve stimulation
Substantia Nigra
Parkinson’s Disease
Drug Therapy
• Improves the functional ability and clinical
status of patients
• Aims at symptomatic relief, does not alter
the disease process
• Patients may have temporary or prolonged
remission
• Side effects can be a problem