Ганглиоблокаторы (Бензогексоний)

Group: Ganglioblokator

Mechanism of action: Blocks H-cholinorecetors of vegetative ganglions, slows down transfer of nervous exaltation with preganglionic on postganglionic fibers. Has oppressing impact on carotid balls and chromaffin tissue of adrenal glands that promotes weakening of reflex pressor influences.

Pharmacological effect: Causes decrease in a AP, a motility GIT, a tone of a bladder, secretion of excretory glands, the accommodation paresis, expands bronchial tubes, increases the CARDIAC CONTRACTIONS RATE.

Indication to use: Obliterating diseases of peripheral arteries (the endarteritis, " alternating" lameness), arterial hypertension (including for knocking over of hypertonic crises), need of carrying out operated hypotension, a peptic ulcer of a stomach and duodenum, chronic gastritis, bronchial asthma (some forms), a diencephalic syndrome.

Side effects: Orthostatic collapse, weakness, dizziness, tachycardia, cardialgia, dryness in a mouth, an accommodation paresis, decrease in memory, an intestines and bladder atony, locks, an ischuria.

Изадрин

1) GROUP: Beta adrenomimetic

2) MECHANISM OF ACTION: Activates adenylatecyclase that leads to accumulation in сells cAMP, influencing system of a protein kinase, depriving a myosin of ability to connect to an actin that interferes with reduction of a smooth musculation and promotes a relaxation of bronchial tubes. Blocks selection by mast cells of volumetric factors (Histaminum and leikotriens), promoting bronchospasm and inflammation development.

3) PHARMOCOLOGICAL EFFECT: Expands bronchial tubes, increases the frequency and force of reductions of heart. Reduces a renal blood-groove, reduces diastolic a AP, increases need of a myocardium for oxygen, expands vessels of an abdominal cavity, skin, mucosas, slows down uterus reductions.

4) INDICATION TO USE: Bronchial asthma (treatment and prophylaxis); bronchial tube obstructive syndrome, pneumosclerosis, AV blockade, attack Morganyi-Adams-Stokes (prophylaxis)

5) SIDE EFFECTS: Hypersensitivity, sharp myocardial infarction, stenocardia, arrhythmias, systemic aterosklerosis. Thyrotoxicosis, pregnancy

Фенобарбитал

1) GROUP: Somnolent (Derivant of barbituric acid)

2) MECHANISM OF ACTION: Interact with allosteric part of GAMKa - bensodiasepin - barbituratic receptoric complex.

Increases affinity of GAMK to GAMKa receptors

Affects induction of microsomal enzymes.

Duration of action depends on speed of getting of body.

3) PHARMOCOLOGICAL EFFECT: In small doses - Somnolent

On large doses - Narcotic

Can be anticonvulsant, antiepileptic

4) INDICATION TO USE: Epilepsy, Spasms, poisoning with chem, Hyperbilirubinemia, Short dreaming

5) SIDE EFFECTS: беспокойство, irritability, vomiting, spasms

Дифенин

1) GROUP: anticonvulsant (Grand Mal 1st line)

2) MECHANISM OF ACTION: Decreases irradiation of epileptic categories on brain centers and through efferent neurones on muscles system due to decreasing in processes power supply of the epileptic categories.

Oppress NAD

Doesn't change normal fucntion of the brain

3) PHARMOCOLOGICAL EFFECT: Membrain stabilising, antiarhythmic, hypotensive action, Antiepileptic action- stabilisation of neuronal membrane body of nerve cell.

4) INDICATION TO USE: Epilepsy, paroxismalic choreatus, miotony, bradyarhytmia, cateterisation of heart.

5) SIDE EFFECTS: hypersensitivity, pregnancy, alcoholism, diabetes - melitus

Психостимуляторы (Кофеина натрия бензоат)

1) GROUP: Psychostimulating substance

2) MECHANISM OF ACTION: blocks central and peripheral A1 and A2 adenosine receptors. Brakes activity of ФДЭ in a CNS, heart, the gladkomyshechnykh bodies, skeletal muscles, fatty tissue, promotes accumulation in them of cAMP and the cGMP (this effect is observed at application of only high doses of a coffeine). Stimulates the medulla centers (respiratory and vasomotor), and also the n.vagus center, has direct stimulating impact on a cerebral cortex. In high doses facilitates intraneuronal conduction in a spinal cord, strengthening spinal reflexes. Increases intellectual and physical serviceability, stimulates mental activity, a physical activity, shortens time of reactions, temporarily reduces exhaustion and a sleepiness.

3) PHARMOCOLOGICAL EFFECT: rendering psychogogic and analeptic effect. In small doses the effect of stimulation, and in larger - effect of depressing of nervous system prevails. Has spasmolytic effect on a smooth musculation(including bronkhodilatiruyushchy effect), on the cross striped - stimulating. Increases secretory activity of a stomach and a diuresis

4) INDICATION TO USE: Decrease in intellectual and physical serviceability, sleepiness, headache of a vascular genesis (including migraine), moderate arterial hypotension, a respiratory depression restitution of necessary level of pulmonary ventilation after use of the common anesthesia. (glaucoma).

5) SIDE EFFECTS: Hypersensitivity (including to other xanthines), alarming frustration acute myocardial infarction, an atherosclerosis), a Bouveret's disease, arterial hypertension, dream violations, at increased fatigue and sleepiness

Транквилизаторы (Мезапам, Диазепам)

1) GROUP: Trancvilisator, anticonvulsant less oppressing CNS

2) MECHANISM OF ACTION: Stimulation of bensodiasepinic receptors of supramolecular GAMK-bensodiasepin-chorionophor recepterd complex.

Stimulate bensodiasepinic receptors, located in allosteric centers in postsynaptic GAMKS centers in postsynaptic GAMK.

Slows down polysynaptic spinal reflexes.

Oppressing of cells of formation encephalon's ствола

3) PHARMOCOLOGICAL EFFECT: sedative-somnolent, anticonvulsant, central miorelaxing action, raises a threshold of painful sensitivity

4) INDICATION TO USE: Dysphory, spasm of skeletal muscles at local trauma, myositis, arthritis, agitation, bursites

5) SIDE EFFECTS: Hypersensitivity, Coma, Shock, Acute alcohol intoxication, myastheny, pregnancy, epylepsy, old age

Нейролептики (Аминазин, Трифтазин, Клозапин)

1) GROUP: Antipsychotic substance

2) MECHANISM OF ACTION: blockade dopamine D2 receptors of mesolimbic and mesocortical system. The antipsychotic effect is shown in elimination of a productive symptomatology of psychoses (nonsense, hallucinations). Stops different types of psychomotor exaltation, reduces psychotic fear, aggression. Sedative action is caused by blockade of adrenoreceptors of a reticular formation of a trunk of a brain. decrease of a spontaneous physical activity, a relaxation of a skeletal musculation, decrease in sensitivity to endogenic and exogenetic incentives at the kept consciousness. At appointment in larger doses there is a dream.

3) PHARMOCOLOGICAL EFFECT: Antipsychotic means (neuroleptic), derivant фенотиазина with an aliphatic side chain. Possesses expressed antipsychotic, sedative, antiemetic, vazodilatiruyushchy (alpha адреноблокирующим), moderate m-holinoblokiruyushchim, and also weak hypothermal action, calms a hiccups; Antiemetic action possesses local irritant action

4) INDICATION TO USE: In psychiatry - psychomotor exaltation (including at patients with schizophrenia); acute crazy states, maniacal and hypomaniacal exaltation at maniac-depressive psychosis, chronic psychosis; mental diseases of various genesis, being accompanied fear, alarm, exaltation, sleeplessness; psychopathy (including at patients with epilepsy and organic diseases of a CNS), alcoholic psychosis. In dermatology - pruritic dermatoses.

5) SIDE EFFECTS: Hypersensitivity, serious cardiovascular illness (arterial hypotension), the expressed depressing of the CNS function and comas of any etiology; progressing general diseases of a head and spinal cord, a peptic ulcer of a stomach and a duodenal in the period of an aggravation (at intake), pregnancy, the lactation period, children's age (till 6 months). Alcoholism (the probability of development of hepatotoxic reactions is increased), pathological changes of blood (hemopoiesis violation), a cancer of a mammary gland

1. Group: antidepressants, monoamine reuptakeinhibitors, nonselective inhibitors (na + 5-ht reuptake inhibitors)

(imipramine (imizine), amitriptyline)

Mechanism of action –

- Blockade transport of serotonin and noradrenalin through the presynaptic membrane

- Resting in synaptic cleft transmitters excite according receptors

They also blockade M-cholinoreceptors, H₁ histamine receptors, α -adrenoreceptors, 5-HT₂ and 5-HT₃ serotonin receptors

§ Structure - tricyclic and tetracyclic

EFFECTS:

§ Timoanaleptic action

the patients are appeared good rite mood

- it is returned optimism, alive aims

- it is disappeared sense of hopelessness and suicidal ideas

§ Timoanaleptic action comes in 10 – 15 days course dose of antidepressants

Additional effects

§ Psychostimulant (in 5-7 days)

§ Sedative

§ Analgesic

§ Hypotermic

§ Antiemetic

IMIPRAMINE (IMIZINE)

§ Timoanaleptic and regulating effects

§ In astheno-depressive syndrome it acts as psycho stimulant

§ In agitative-depressive syndrome predominates antianxiety and sedative action

§ It is more effective by depression in the combination with asthenia

Indications for use. Prescribed for depression and anxiety and depressive states of various origins (manic-depressive illness, schizophrenia, reactive and neurotic depression, bedwetting, etc.).

When ingested toxic doses of these substances are absorbed in the gut after 30-60 minutes after intramuscular administration - after 5-10 min. Maximum concentration in the blood after administration of therapeutic doses of 1.5-2 hours is observed drug levels in plasma are relatively low due to their rapid deposition in tissues, preferably parenchymal organs (spleen, liver, adrenal gland, lung, brain, kidney, intestinal wall, the myocardium, etc.).

AMITRIPRYLINE

– Timoanaleptic with sedative properties

- It is prescribed to patients with agitative-depressive syndrome

- Blockades M-cholinoreceptors

Amitriptyline (triptizol) also applies to drugs with good bioavailability and a high affinity for plasma proteins. The half-life in healthy subjects is 24-48 hours, and patients it ranges from 9 to 24 hours Therapeutic concentration of amitriptyline in blood is 0, 04-0, 16 g / ml. The drug is extensively metabolized in the liver, becoming the norm and dinitrotriptilin having antidepressant properties. Two of these metabolites as well as hydroxy and N- oxides are excreted in the urine: 2 weeks in this way 80 % of the metabolites derived.

The main indication for the use of antidepressants taking into account their pharmacodynamics are depressive states. In depressive states, accompanied by apathy, lethargy, lack of initiative, apply Nialamidum - 50-70 mg / day in the morning and afternoon.

- There are differences in the indications for use of other antidepressants. With antidepressant imipramine has an effect when the motor and ideatornoy retardation, involutive climacteric, reactive, alcohol depression. This eliminates the feeling of depression, improves mood, alertness appears, decreases motor retardation. Assign it orally at a dose of 75-100 mg / day with gradual increase it up to 200-250 mg / day. Children under 1 year old (and older people) get a dose of 100 mg / day, which doubles every 7 years of life. Amitriptyline is prescribed for the same indications starting from 50-75 mg / day.

SIDE EFFECTS of NONSELECTIVE REUPTAKE INHIBITORS

§ Disorders of CNS – headache, anxiety, alarm,

mental confusion, desorientation, delirium, hallucination, nightmare, ataxia, tremor, paraesthesia

§ Cardiotoxicity – decrease of heart rate, tachycardia,

arythmia

§ Postural hypotension

§ Peripheral M-cholinoblocking action – dry mouth, mydriasis, increase IT, accommodative paralysis and etc.

§ Agranulocytosis, thrombocytopenia, increased the body

mass (in long prescription)

§ Rashes and jaundice