RESERPIN penetrates well through the BBB, causing depression of the central nervous system. Therefore, it can cause lethargy, drowsiness, depression, decreased potency, with prolonged use - drug parkinsonism
OCTADINE does not affect the central nervous system. Its hypotensive effect is more pronounced, orthostatic collapse is possible (after taking the drug, it is necessary to be in a horizontal position for 1.5 - 2 hours)
Indications: Both drugs are used for the systematic treatment of arterial hypertension.
Side effects:
Common to OCTADINE and RESERPINE:
• dizziness
• general weakness
• bradycardia
• swelling of the nasal mucosa
• increased secretion of the digestive glands (possible ulcerogenic effect)
• increased gastrointestinal motility (diarrhea is possible)
• sodium and water retention (it is recommended to combine with diuretics)
Additionally: RESERPIN - depression of the central nervous system
OCTADINE - orthostatic hypotension
• Contraindications: Severe organic cardiovascular diseases with symptoms of decompensation, severe bradycardia, pronounced atherosclerosis, gastric ulcer and duodenal ulcer, renal failure, lactation period
• Do not prescribe drugs (hypertensive crisis is possible):
1. With pheochromocytoma
2. Together with MAO inhibitors
3. Together with tricyclic antidepressants
Comparative characteristics: ORNID (bretilium tosylate)
• The mechanism of action is associated with the stabilization of the presynaptic membrane and blocking the release of the mediator into the synaptic cleft. The hypotensive effect of the drug is not sufficiently pronounced for clinical use, but the antiarrhythmic effect is clearly manifested, mainly in ventricular arrhythmias (especially those resistant to other drugs)
• Side effects: nephrotoxicity, orthostatic hypotension, fever, weakness, swelling of the nasal mucosa
• Contraindications: hypotension, acute cerebrovascular accident, severe renal failure
METHYLDOPA (aldomet, dopegit)
The drug penetrates well into the central nervous system and, integrating into the synthesis chain of the mediator, promotes the formation of methylnorepinephrine, which stimulates (and is stronger than the true mediator) 2-adrenergic receptors of inhibitory neurons in the central nervous system
This leads to an increase in inhibitory effects on sympathetic impulses to the heart and blood vessels (the action is similar to CLOFELINE, see), as a result of which the vessels expand, the total peripheral vascular resistance decreases and bradycardia develops
Causes sedation Orthostatic hypotension is rare
• It is used for arterial hypertension
• Side effects: general weakness, dyspeptic disorders, redness of the upper half of the trunk (due to vasodilation), reversible leukopenia and thrombocytopenia, hemolytic anemia, liver dysfunction with cholestasis and jaundice (control blood and liver function!). Retention of sodium and water (must be combined with diuretics!)
• Contraindications: diseases of the blood system (leukopenia, agranulocytosis, thrombocytopenia, hypo- and aplastic anemias), liver (hepatitis, cirrhosis), pheochromocytoma
3. Preparations of adrenal cortex hormones (glucocorticoids, mineralocorticoids). Classification. Mechanism of action. Indications for use. Side effects. Contraindications Comparative evaluation of drugs.
Classification:
Mineralocorticoids: Aldosterone, 11-Deoxycorticosterone, 11-Desaxi-17-hydroxycorticosterone
Glucocorticoids: I. Preparations of natural hormones and their esters: CORTISONE, HYDROCORTISONE
II. Synthetic drugs: 1) Inhalation:
TRIAMCINOLONE (azmacort)
FLUNISOLID (ingacort)
BECLOMETAZONE (beclomet, becotide)
BUDESONID (pulmicort, benacort)
FLUTICAZONE (flixotide)
2) System:
Prednisolone (decortin, medopred)
METHYLPEDNIZOLONE (metipred)
BETAMETAZONE (celeston)
DEXAMETHAZONE (dexona, dexazone)
TRIAMCINOLON (berlikort, kenalog)
3) Local action:
FLUMETAZONE PIVALATE ("lokakorten" "lorinden")
FLUOCINOLONE ACETONIDE ("sinaflan", "sinalar")
BUDESONID (apulein)
HALOMETAZONE (sicorten)
BETAMETAZONE ("diprolene", "celestoderm")
Mechanism of action: Mineralocorticoids: Increase the reabsorption of sodium and water, at the same time increase the secretion of potassium and magnesium ions, calcium in the renal tubules.
GLUCOCORTICOIDS:
1. Anti-inflammatory
2. Antiallergic and immunosuppressive
3. Anti-shock
Anti-inflammatory:
1. Suppression of the production of prostaglandins, leukotrienes and platelet activating factor due to inhibition of phospholipase A2.
2. Inhibition of hyaluronidase activity.
3. Decreased permeability and increased resistance of capillary walls, cell membranes and subcellular structures.
4. Delayed development of connective tissue.
5. Decrease in the number of leukocytes in the area of inflammation.
6. Suppression of the activity of macrophages and fibroblasts.
7. Inhibition of cyclooxygenase-2 activity
Antiallergic:
1. Decrease in the activity of T- and B-lymphocytes.
2. Inhibition of antibody synthesis.
3. Suppression of the release of histamine, serotonin, acetylcholine.
4. Increased activity of histaminase and cholinesterase.
5. Slowdown in the development of lymphoid tissue.
6. Suppression of production of interleukins and other cytokines.
Anti-shock:
1. Potentiation of the action of vasopressor substances (angiotensin, adrenaline, norepinephrine) and an increase in blood pressure.
2. Improving the work of the heart.
Indications: Mineralocorticoids:
1. Addison's disease (chronic adrenal insufficiency).
2. Hypotension with orthostatic disorders.
3. Myasthenia gravis.
4. Adynamia.
5. Hypochloremia.
Glucocorticoids: Inflammatory diseases of an infectious and allergic nature (rheumatism, systemic lupus erythematosus, collagenoses, rheumatoid arthritis, generalized dermatitis, eczema, neurodermatitis, psoriasis, etc.).
2. Severe infectious diseases occurring with high fever and intoxication (diffuse peritonitis, meningitis, typhoid fever).
3. Severe allergic and toxic-allergic conditions (anaphylactic shock, reaction to a blood transfusion of another group, acute hemolytic anemia, bronchial asthma, etc.).
4. Shock states.
5. Malignant diseases of the hematopoietic organs (leukemia, lymphogranuloma, etc.).
Side effects: Mineralocorticods: 1. Edema.
2. Arterial hypertension.
3. Hypokalemia (impaired heart function, arrhythmias).
4. Allergic reactions.
5. Development or worsening of heart failure.
Glucocorticoids: Withdrawal syndrome and acute adrenal insufficiency (with abrupt withdrawal of drugs).
2. Itsenko-Cushing's symptom complex (edema, arterial hypertension, obesity, "moon face", "bovine hump").
3. Hyperglycemia (steroidal diabetes).
4. Osteoporosis, multiple caries.
5. Slowing down the regeneration processes (slowing down the healing of wounds, fractures).
6. Decrease in resistance to infections, exacerbation of a dormant infection.
7. Violation of the menstrual cycle, impotence.
8. Ulceration of the gastric mucosa, exacerbation of peptic ulcer disease.
Contraindications: Mineralocorticoids: 1. Acute and chronic heart failure.
2. Arterial hypertension.
3. Atherosclerosis.
4. Cirrhosis of the liver.
5. Jade.
Glucocorticoids: 1. Severe hypertension.
2. Itsenko-Cushing's disease.
3. Pregnancy.
4. Insufficiency of blood circulation of the III degree.
5. Acute endocarditis.
6. Psychoses.
7. Osteoporosis.
8. Peptic ulcer of the stomach and duodenum.
9. Active forms of tuberculosis
Antiviral drugs are a group of drugs used for the prevention and treatment of viral infections.
Classification:
- antiherpetic - acyclovir, valacyclovir, penciclovir and famciclovir
- anti-cytomegalovirus - ganciclovir, valganciclovir, foscarnet and cidofovir.
- anti-influenza - amantadine, rimantadine - and viral neuroaminidase inhibitors - zanamivir, oseltamivir
- extended spectrum drugs - ribavirin, lamivudine.
- antiretroviral (for the prevention and treatment of HIV infection) - 1. Nucleoside inhibitors of HIV reverse transcriptase.
2. Non-nucleoside inhibitors of HIV reverse transcriptase.
3. Inhibitors of HIV protease.
Mechanism of action: Antiherpetic chemotherapy
Acyclovir is the ancestor of antiherpetic drugs - blockers of viral DNA synthesis. The active metabolite of acyclovir, acyclovir triphosphate, has an antiviral effect. By inhibiting viral DNA polymerase, acyclovir triphosphate blocks viral DNA synthesis.
Penciclovir in human cells affected by the virus is activated, turning into penciclovir triphosphate, which disrupts the synthesis of viral DNA.
Foscarnet forms inactive complexes with DNA polymerase of herpes viruses and cytomegaloviruses.
Anti-cytomegalovirus: Ganciclovir.
In cells affected by cytomegalovirus, ganciclovir is converted to its active form - ganciclovir triphosphate, which inhibits viral DNA polymerase.
Anti-influenza:
The antiviral effect of amantadine and remantadine is realized by blocking special ion channels of the M2-channels of the influenza A virus, and therefore its ability to penetrate cells and release ribonucleoprotein is impaired. Thus, the most important stage of viral replication is inhibited.
Extended spectrum drugs: RIBAVIRIN.
The mechanism of antiviral action has not yet been clarified. It is assumed that ribavirin causes a decrease in the intracellular pool of guanosine triphosphate and, thus, indirectly decreases the synthesis of viral nucleic acids.
Lamivudine.
In cells affected by the virus, it is activated, turning into lavimvudine triphosphate, which inhibits hepatitis B virus DNA polymerase and HIV reverse transcriptase.
Antiretrovirals: The structure of all nucleic reverse transcriptase inhibitors is based on one of the analogs of the natural nucleoside (thymidine, adenine, cytidine or guanine), which determines the general properties of the metabolites of each drug to block HIV reverse transcriptase and selectively inhibit viral DNA replication. Under the action of appropriate enzymes, drugs are metabolized to form triphosphates, which exhibit pharmacological activity. The ability of drugs in this group to inhibit HIV reverse transcriptase is hundreds of times higher than the ability to inhibit human DNA polymerase. Nucleoside reverse transcriptase inhibitors are active in HIV-infected T cells and macrophages, inhibiting the early stages of the virus life cycle.
Nature and spectrum of action: Antiherpetic: Acyclovir - Spectrum of action: Herpes symplex types 1 and 2, Varicella-zoster, cytomegalovirus (470 times less sensitive to acyclovir than HSV type 1). Mode of action: virucidal.
Anti-cytomegalovirus
Ganciclovir
Spectrum of activity: cytomegalovirus (activity is 10-50 times higher than that of acyclovir), herpes viruses. Character: virucidal
Anti-influenza drugs
Remantadine
Spectrum of action - type A influenza virus. Nature: virucidal.
Extended-spectrum antivirals
Ribavirin
Structurally similar to the guanosine nucleotide. Possesses a wide spectrum of activity against many DNA and RNA viruses. Highly toxic. Character: virucidal.
INDICATIONS:
Antiherpetic: Valacyclovir:
- infections of the skin and mucous membranes;
- ophthalmic herpes (only acyclovir);
- genital herpes;
- herpetic encephalitis;
- neonatal herpes.
Anti-cytomegalovirus: cytomegalovirus infection
Anti-influenza: Amantadine and rimantadine- Treatment of influenza caused by virus A.
Prevention of influenza (if the epidemic is caused by the A virus). Efficiency - 70 - 90%.
Extended spectrum drugs: Ribavirin - Respiratory syncytial virus infections (only serologically confirmed): severe bronchiolitis and pneumonia in infants and young children at risk of death (congenital heart disease, immunodeficiency, bronchopulmonary dysplasia), in the background severe cystic fibrosis or pulmonary hypertension.
Antiretrovirals:
Non-nucleoside reverse inhibitors
HIV transcriptase
Combination therapy for HIV-1 infection (nevirapine, efavirenz).
Prevention of mother-to-newborn transmission of HIV-1 infection (nevirapine).
Chemoprophylaxis of parenteral HIV infection (efavirenz).
Side effects:
Antiherpetic: Acyclovir: Local:
- burning sensation when applied to mucous membranes, especially when applied vaginally;
- phlebitis when administered intravenously.
Systemic:
Gastrointestinal tract: pain or discomfort in the abdomen, nausea, vomiting, diarrhea;
Anti-cytomegalovirus: Ganciclovir: Hematological reactions (up to 40%): neutropenia, anemia, thrombocytopenia. Cases of severe persistent neutropenia complicated by fatal infection have been reported. Risk factor: AIDS.
Gastrointestinal tract: diarrhea (44%), anorexia, vomiting.
Anti-influenza:
Gastrointestinal tract: abdominal pain, impaired appetite, nausea.
CNS: when using amantadine - in 14% of patients, remantadine - in 3 - 6%: drowsiness, insomnia, headache, dizziness, visual disturbances, irritability, paresthesia, tremors, convulsions.
Extended spectrum drugs: Ribavirin: Hematological reactions: anemia, hemolytic anemia, leukopenia, neutropenia, granulocytopenia, trombocytopenia. Control methods: clinical blood test every 2 weeks.
CNS: asthenic syndrome, headache, insomnia, fatigue, irritability.
Antiretrovirals:
• Diarrhea
• Fatigue
• Headache
• Liver problems
• Upset stomach (nausea), stomach pain, vomiting, decreased appetite
Contraindications: Antiherpetic: Valacyclovir: Allergic reactions, hypersensitivity to the drug.
Anti-cytomegalovirus: Undesirable side effects in 1/3 of patients are the reason for drug withdrawal
Anti-influenza: Arbidol.
Allergic reaction to arbidol.
Age up to 2 years (in children from 2 to 6 years, it is used only for the treatment of influenza).
Extended spectrum drugs: Ribavirin: Hypersensitivity to ribavirin.
Severe hepatic and / or renal impairment.
Anemia
Hemoglobinopathy.
Severe heart failure.
Pregnancy.
Antiretrovirals: STAVUDIN (D4T).
- hypersensitivity to stavudine;
- peripheral neuropathy;
- lactation;
- age up to 3 months;
- liver failure;
- severe renal failure