General pharmacology. Reactions of the body to the repeated administration of drugs Accumulation of the substance during repeated administrations
a perverted reaction of the body to the introduction (even once) of a medicinal substance
hypersensitivity of the body to the drug
23. The accumulation of drugs in the body with repeated injections is called:
material cumulation
functional cumulation
sensitization
24. Sensitization underlies:
1. allergies
2. idiosyncrasy
3. tachyphylaxis
4. cumulation
25. A sign of addiction to LP is called:
feeling better after taking the medicine
increased sensitivity of the body to the drug
irresistible urge to take a drug
insomnia
26. Next to the name of the dose, indicate its definition
Dose name Dose definition:
coursework a) the amount of the substance at one time
single b) dose that has a therapeutic effect
daily allowance d) the number of drugs for the course of treatment
4. toxic c) the amount of drugs to be taken during the day
5. Therapeutic e) the amount of drug that causes dangerous
toxic effects on the body
27. The dose of the drug for a 3-year-old child is:
1/24 adult dose
1/12 adult dose
1/3 adult dose
1/8 adult dose
28. Combine:
Negative action type Definition
1. teratogenic a) malformation of the fetus
2. mutagenic b) stimulation of growth of malignant
3. carcinogenic tumors
4. ulcerogenic c) ulceration of the mucous membrane of the stomach
d) damage to the cell of the genetic appa-
29. Combine:
Term Definition
1. tachyphylaxis a) an irresistible urge to repeat
2. drug dependence taking drugs
3. sensitization b) severe and somatic disorders
4. withdrawal syndrome of the body, after a sudden cessation
reception of drugs
c) increasing the sensitivity of the organization
ma to action lv
d) a rapid weakening of the effect of the drug when
re-introduction
30. Absorption of most of the drug occurs:
in the oral cavity
in the stomach
in the small intestine
in the large intestine
31. Which substances penetrate the cell membrane more easily:
1. lipophilic
2. hydrophilic
32. Combine:
1. antagonist a) interaction with the receptor, causes
effect less than maximum
2. agonist b) interaction with the receptor, causes
maximum effect
3. partial agonist c) blocks the receptor
4. agonist-antagonist d) interacts with receptors; stimulus-
lyates one subtype of the receptor and blocks
no other subtype
33. Release of a drug from the body is called:
1. elimination
2. excretion
3. metabolism
4. esterification
34. The main routes of drug excretion from the body include:
intestines
mammary gland
35. The predominant implementation of the biotransformation of most drugs in the body:
36. The drug undergoes the greatest breakdown in the liver when it is administered:
into the rectum
37. Oil solutions cannot be entered:
1. intramuscularly
2. intravenously
3. inhalation
4. subcutaneously
38. Side effect LP is:
action expected by the doctor
dose-dependent effect
unwanted action that interferes with the manifestation of the main action
A) Accumulation: dose, interval between doses and fluctuations in the concentration of the drug in. In many diseases, successful drug therapy is possible only if the concentration of the drug is maintained at a constant high level.
This means the need regular drug intake and adherence to a regimen in which the plasma concentration of the substance does not fall below the therapeutically effective value and does not exceed the minimum toxic concentration. However, a constant level of a substance in the blood is undesirable if it contributes to a decrease in the effectiveness of the drug (the development of resistance to it) or if it is needed in the blood only at certain periods of time.
sustainable blood concentration can be achieved by prescribing the drug in the form of long-term intravenous infusions; the height of the state of equilibrium is determined by the rate of infusion. This procedure is often used in a hospital setting, but in outpatient settings unfeasible. When administered orally, a compromise is the division of the total daily dose into several doses.
In that case when daily dose given in several doses, the concentration of the drug in the blood varies slightly.
As shows practice, patients often violate the regimen of taking the drug, especially in cases where it is required to take it several times a day (the so-called non-compliance with the patient's doctor's prescriptions). Fluctuations in the concentration of the drug in the blood between doses are less pronounced if the drug is given in a prolonged form.
If a drug taken for a long time and often, the time required to reach the equilibrium of the accumulation of the substance depends on the rate of elimination. It has been empirically established that the plateau is reached in a time approximately equal to three t 1/2 .
At drugs with slow elimination, intensively accumulating in the body (phenprocoumon, digitoxin, methadone), the optimal concentration in the blood is achieved for a long time. e. increasing the initial (saturating) dose accelerates the achievement of equilibrium, which is subsequently maintained by taking lower (maintenance) doses.
For substances with slow excretion, 1 dose per day may be sufficient to maintain a stable blood concentration.
b) Elimination changes in progress drug therapy . It is important to understand that for drugs taken regularly and accumulating in the blood to the desired level, the conditions for biotransformation and excretion do not always remain constant. Excretion may be accelerated as a result of enzyme activation or changes in urine pH.
In this case equilibrium concentration in the blood decreases to a new value, depending on the withdrawal speed. The effect of the drug may be weakened or stopped. And vice versa, when excretion is impaired (with progressive kidney failure), the average concentration in the blood of drugs excreted by the kidneys increases and can reach toxic levels.
1. Routes of administration medicinal substances into the body, their absorption, distribution, transformation, excretion studies:
A. Pharmacodynamics.
B. + Pharmacokinetics.
B. Private pharmacology.
G. Pharmacotoxicology.
2. The process of accumulation of medicinal substances in the body is called:
A. + Cumulation.
B. Synergy.
B. Antagonism.
D. Drug addiction.
3. A drug with an irritating effect:
A. De-nol.
B. + Mustard plasters.
W. Venter.
G. Activated carbon.
4. A drug with an adsorbing effect:
A. Menovazin.
B. + Activated carbon.
V. Novocain.
G. Diphenhydramine.
5. Disease in which pilocarpine hydrochloride is used:
A. Hypertension.
B. + Glaucoma.
B. Myopia.
G. Atony of the intestine.
6. Atropine sulfate is contraindicated in:
A. Peptic ulcer of the stomach.
B. + Glaucoma.
B. Bronchial asthma.
D. Spasms of the stomach.
7. Drug used for rhinitis:
A. + Galazolin.
B. Bisacodyl.
B. Aceclidine.
G. Scopolamine.
8. Analogue of promedol:
A. Panadol.
B. + Omnopon.
V. Solpadein.
G. Voltaren.
9. Possible complication when using aspirin:
A. Diarrhea.
B. + Ulcerogenic effect (ulceration of the gastrointestinal mucosa).
B. Change in heart rate.
10. The main pharmacotherapeutic action of paracetamol:
A. + Antipyretic.
B. Anti-inflammatory.
B. Antirheumatic.
G. Antiarrhythmic.
11. Narcotic analgesics are used for pain:
A. Golovnykh.
B. Articular.
V. Dental.
G. + Oncological.
12. Pharmacological group elenium:
A. + Tranquilizers.
B. Sleeping pills.
B. Expectorants.
D. Antihistamines.
13. Pharmacological group of motherwort tincture:
A. General tonic.
B. + Sedatives.
B. Sleeping pills.
D. Antihistamines.
14. Pharmacological group of ginseng tincture:
A. Sedatives.
B. Sleeping pills.
B. + General tonic.
D. Antihypertensive drugs.
15. A drug used to stop an attack of angina pectoris:
A. Nitrosorbide.
B. + Nitroglycerin.
V. Sustak-forte.
G. Nitrong.
16. Antispasmodic myotropic action:
A. Hypothiazide.
B. + Papaverine hydrochloride.
V. Codeine.
G. Mezaton.
17. Indication for the use of strophanthin-K:
A. + Acute heart failure.
B. Hypertensive crisis.
B. Chronic heart failure.
G. Neuroses.
18. Cardiac glycoside for the treatment of chronic heart failure:
A. + Digitoxin.
B. Korglikon.
V. Strofantin-K.
D. Nitroglycerin.
19. Pharmacological group of furosemide:
A. Antitussives.
B. + Diuretics.
B. Antihistamines.
D. Laxatives.
20. Opioid antitussive:
A. Libeksin.
B. Mukaltin.
B. + Codeine.
G. Bronchikum.
21. Atrovent is prescribed for:
A. + Bronchial asthma.
B. Myasthenia gravis.
B. Hypotension.
G. Renal colic.
22. Antihistamine blocking H 1 receptors:
A. Hydrocortisone.
B. Ephedrine.
B. + Diazolin.
G. Salbutamol.
23. A drug with a choleretic effect:
A. Pepsin.
B. + Holenzim.
B. Gastric juice.
G. Smecta.
24. Antacid:
A. + Almagel.
B. Acidine-pepsin.
V. Flamin.
G. Senade.
25. A drug with a laxative effect:
A. No-shpa.
B. + Bisacodyl.
V. Dibazol.
26. Actrapid is used for:
A. Treatment of myxedema.
B. Treatment of Graves' disease.
B. + Treatment of diabetes.
D. Treatment of cretinism.
27. Ascorbic acid is used for:
A. Rakhite.
B. Pellagre.
V. + Tsinge.
G. Hemorrhagic diathesis.
28. When using levomycetin, it is possible:
A. Ototoxic effect.
B. Effect on vision.
B. + Inhibition of hematopoiesis.
G. Action on the central nervous system.
29. Antibiotic used for candidomycosis:
A. Levomycetin.
B. + Nystatin.
B. Benzylpenicillin.
G. Tetracycline.
30. The group of fluoroquinolones includes:
A. Claforan.
B. + Ofloxacin.
B. Amikacin.
G. Trichopolum.
31. The breadth of therapeutic action is the range of doses:
A. From medium therapeutic to minimal toxic.
B. + From minimal therapeutic to minimal toxic.
B. From minimal therapeutic to minimal lethal.
D. From minimal toxic to lethal.
32. Bioavailability of a medicinal product is:
A. The time it takes for the drug concentration in the blood to decrease by 50%.
B. The process of transformation of matter in the body.
D. The totality of the processes of biotransformation and excretion.
33. Inductors are medicines:
A. + Increasing the activity of liver enzymes.
B. Lowering the activity of liver enzymes.
B. Blocking specific receptors.
D. Excitatory specific receptors.
34. You can not enter intravenously:
A. + Suspensions.
B. Hypertonic solutions.
B. Hypotonic solutions.
D. Aqueous solutions.
35. Increasing the body's sensitivity to a medicinal substance during its repeated administration is:
A. Habituation.
B. Addiction.
B. + Sensitization.
D. Synergy.
36. The effect of the drug, causing deformities of the fetus:
A. Embryotoxic.
B. Ototoxic.
B. + Teratogenic.
G. Nephrotoxic.
37. Decreased sensitivity of the body to a medicinal substance with its repeated administration:
A. Synergism.
B. Sensitization.
B. Antagonism.
G. + Addictive.
38. In case of antagonism, the effect of the action of medicinal substances:
A. Increases.
B. + Decreases.
B. Does not change.
G. Potentiated.
39. Irresistible urge to take medication:
A. Abstinence.
B. Addictive.
B. + Drug addiction.
D. Cumulation.
40. The mechanism of action of enveloping agents:
A. Blockade of sensitive receptors.
B. + Formation of a protective colloidal film.
B. Adsorption of chemical compounds on its surface.
41. The mechanism of action of adsorbing agents:
A. + Adsorption of chemical compounds on its surface.
B. Blockade of sensitive receptors.
B. Formation of a protective colloidal film.
42. Preparations from the group of local anesthetics:
1. Novocain.
2. Anestezin.
4. Lidocaine.
A. True 1,2,3.
B. True 2.4.
B. + True 1,2,4.
G. True 3.4.
43. Drugs used for rhinitis:
1. Galazolin.
2. Alupent.
3. Papaverine hydrochloride.
4. Sanorin.
A. True 1.2.
B. True 1.3.
B. + True 1.4.
G. True 2.3.
44. Preparations with astringent properties:
2. Anestezin.
3. Bismuth subnitrate.
4. Menthol.
A. + True 1.3.
B. True 2.4.
B. True 1.2.
G. True 3.4.
45. Drugs that have an irritating effect:
1. Menthol.
3. Mustard plasters.
4. Novocain.
A. True 1.2.
B. + True 1.3.
B. True 2.4.
G. True 3.4.
46. Indications for the use of M-cholinomimetics:
1. Myasthenia.
2. Glaucoma.
3. Epilepsy.
4. Atony of the intestine.
A. True 1.2.
B. True 2.3.
B. + True 2.4.
G. True 1.4.
47. Drugs used to treat glaucoma:
1. Atropine sulfate.
2. Pilocarpine hydrochloride.
3. Ocupress.
4. Naphthyzin.
A. True 1.2.
B. True 1.4.
B. + True 2.3.
G. True 1.3.
48. Complications arising from the use of atropine:
A. Cumulation, skin rashes, runny nose and cough, conjunctivitis.
B. + Accommodation paralysis, increased intraocular pressure, dry mouth, atony
intestines.
49. Indications for the use of atropine sulfate:
1. Atony of the intestine.
2. Bronchial asthma.
3. Glaucoma.
4. Spasms of smooth muscles of the gastrointestinal tract.
A. True 1.2.
B. True 2.3.
B. + True 2.4.
G. True 3.4.
50. Side effect of anaprilin:
A. + Bronchial spasm.
B. Parkinson's syndrome.
B. Gastric and duodenal ulcer.
D. Excitation of the central nervous system, insomnia.
51. A drug with a vasoconstrictive effect:
A. Pilocarpine hydrochloride.
B. + Adrenaline.
V. Anaprilin.
G. Atropine.
52. Anticholinergics include all of the listed drugs, except:
A. + Pilocarpine.
B. Platifillina.
V. Atropine.
G. Gastrocepin.
53. The action of ephedrine:
B. + Has a vasoconstrictor and bronchodilatory effect, excites the central nervous system.
54. Beta-adrenergic stimulant:
A. Mezaton.
B. + Izadrin.
V. Naphthyzin.
G. Galazolin.
55. There is no naphthyzine in the pharmacy. It can be replaced:
A. Anabazin.
B. Metacin.
V. Astmopent.
G. + Galazolin.
56. Blood pressure is increased by all of the listed drugs, except:
A. Mezaton.
B. Adrenaline.
V. + Izadrina.
G. Norepinephrine.
57. Antihypertensive drugs from the group of sympatholytics:
1. Reserpine.
2. Pyrilene.
3. Eufillin.
4. Adelfan.
A. True 1.2.
B. True 2.3.
B. True 3.4.
D. + True 1.4.
58. Indications for the use of adrenaline hydrochloride:
1. Insomnia.
2. Bronchial asthma.
3. A sharp decrease in blood pressure.
4. Rheumatism of the joints.
A. + True 2.3.
B. True 1.4.
B. True 2.4.
G. True 1.3.
59. Beta-blockers are used for:
A. Hypotension.
B. Atony of the intestine.
B. + Angina pectoris.
G. Diabetes mellitus.
60. For inhalation anesthesia use:
A. Sodium hydroxybutyrate.
B. Geksenal.
B. + Nitrous oxide.
G. Propanidid.
61. Hypnotic drugs that change the structure of sleep:
A. Antihistamines.
B. + Barbiturates.
B. Tranquilizers.
D. Derivatives of the aliphatic series.
62. Pharmacological group of phenobarbital:
A. Tranquilizers.
B. + Sleeping pills.
B. Expectorants.
D. Antihistamines.
63. Sleeping pills from the group of benzodiazepines:
1. Nitrazepam.
2. Nembutal.
3. Phenazepam.
4. Imovan.
A. True 2.3.
B. True 1.4.
B. + True 1.3.
G. True 2.4.
64. When insomnia is prescribed:
1. Promedol.
2. Nitrazepam.
3. Donormil.
4. Imovan.
A. True 1.2.
B. True 1.3.
B. + True 2,3,4.
G. True 1,3,4.
65. In Parkinson's disease, the following is prescribed:
A. Phenobarbital.
B. Suxilep.
B. + Levodopa.
G. Konvuleks.
66. Side effects of neuroleptics:
A. Cumulation.
B. Ototoxicity.
B. Withdrawal syndrome.
G. + Phenomena of parkinsonism.
67. Child 3 years old at elevated temperature appoint:
A. Aspirin.
B. Indomethacin.
V. Citramon.
G. + Paracetamol.
68. Long-acting opioid analgesic:
A. Codeine phosphate.
B. + Morfilong.
V. Estotsin.
G. Pentalgin.
69. Cancer patients with severe pain appoint:
A. + Morphine.
B. Aspirin.
B. Paracetamol.
G. Ortofen.
70. Opioid analgesics:
1. Promedol.
2. Panadol.
3. Omnopon.
4. Butadion.
A. True 1.2.
B. True 2.3.
B. True 3.4.
D. + True 1.3.
71. Indications for the use of narcotic analgesics:
1. Articular, rheumatic pains.
2. Traumatic pain.
3. Pain in malignant tumors.
4. Toothache, headache.
A. True 1,2,4.
B. True 2.4.
B. + True 2.3.
G. True 1.4.
72. Voltaren is used:
A. + When rheumatoid arthritis, inflammation of the joints.
B. With chronic constipation.
D. For infections respiratory tract, urinary tract, gastrointestinal tract.
73. Non-steroidal anti-inflammatory drugs are used for:
A. Traumatic pains.
B. Myocardial infarction.
B. + Rheumatism.
G. Cardiogenic shock.
74. Mechanism of action of non-steroidal anti-inflammatory drugs:
A. + Block the production of inflammatory mediators.
B. Inhibit metabolic processes.
B. Stimulate metabolic processes.
D. Block nerve endings.
75. Another name for indomethacin:
A. Diclofenac.
B. Ibuprofen.
B. + Metindol.
G. Maxigan.
76. To reduce the ulcerogenic effect of aspirin:
1. Assign before meals.
2. Assign after a meal.
3. Wash down with juice.
4. Grind.
A. True 2.3.
B. True 1.3.
B. + True 2.4.
G. True 3.4.
77. When are NSAIDs used?
1. Fever, fever.
2. Pain in malignant tumors.
3. Rheumatic, joint pains.
4. Headache.
A. True 1.2.
B. + True 1,3,4.
B. True 2,3,4.
G. True 3.4.
78. Neuralgia, arthritis, rheumatism is treated with:
1. Ibuprofen.
2. Fentanyl.
3. Diclofenac sodium.
4. Ketoprofen.
A. True 1,2,3.
B. + True 1,3,4.
B. True 2.4.
G. True 1.2.
79. Antipsychotic action has:
A. Diazepam.
B. + Aminazin.
V. Corvalol.
G. Fentanyl.
80. For treatment acute psychoses appoint:
A. Sedatives.
B. Nootropics.
B. + Antipsychotics.
D. Tranquilizers.
81. For depression apply:
A. + Amitriptyline.
B. Piracetam.
B. Caffeine.
G. Chlosepides.
82. The group of tranquilizers includes:
1. Elenium.
2. Phenobarbital.
3. Seduxenus.
4. Indomethacin.
A. + True 1.3.
B. True 2.4.
B. True 2.3.
G. True 3.4.
83. Tranquilizer that does not cause drowsiness:
A. Chlosepides.
B. Oxazepam.
B. + Medazepam.
G. Diazepam.
84. Complications arising from the use of bromine preparations:
A. + Cumulation, skin rashes, runny nose and cough, conjunctivitis.
B. Accommodation paralysis, increased intraocular pressure, dry mouth, atony
intestines.
B. Allergy, teratogenic effect, defeat bone tissue and tooth enamel.
D. Increase in blood pressure for 1.5-2 hours after the initial use of the drug.
85. Pharmacological group of valerian tincture:
A. Sleeping pills.
B. Antihistamines.
B. General tonic.
G. + Sedatives.
86. Sedatives:
1. Persen.
2. Eleutherococcus tincture.
3. Novo - Passit.
4. Corvalol.
A. True 1,2,3.
B. + True 1,3,4.
B. True 2.3.
G. True 1.4.
87. Sedatives:
1. Caffeine.
2. Valerian tincture.
3. Tincture of motherwort.
4. Sodium bromide.
A. True 1,2,3.
B. True 1.4.
B. + True 2,3,4.
G. True 3.4.
88. Sedative drug that causes cumulation:
A. Novopassit.
B. Corvalol.
B. + Sodium bromide.
G. Motherwort tincture.
89. A drug that promotes concentration, improves memory, facilitates learning:
A. Haloperidol.
B. Grandaxin.
B. Amitriptyline.
G. + Nootropil.
90. Caffeine:
A. It has a central, direct and reflex coronary dilating effect.
B. + Increases mental and physical performance, eliminates fatigue.
G. Inhibits synthesis folic acid causes crystalluria of the kidneys.
91. Side effects of caffeine:
A. Cumulation.
B. Drowsiness.
B. + Insomnia.
G. Decrease in working capacity.
92. Another name for piracetam:
A. Phenibut.
B. Picamilon.
V. Aminalon.
G. + Nootropil.
93. Psychostimulants are used:
1. In shock.
2. With narcolepsy (pathological drowsiness).
3. During the collapse.
4. To improve mental and physical performance.
A. True 1,2,4.
B. True 2,3,4.
B. + True 2.4.
G. True 1.2.
94. General tonic plant origin:
1. Tincture of Aralia.
2. Ginseng tincture.
3. Valerian tincture.
4. Tincture of motherwort.
A. True 1.3.
B. + True 1.2.
B. True 1.4.
G. True 3.4.
95. For the treatment of bronchial asthma, the following are used:
2. Galazolin.
3. Orciprenaline sulfate (alupent).
4. Fenoterol.
A. True 2.3.
B. True 1.4.
B. True 2.4.
D. + True 3.4.
96. Pharmacological group of tavegil:
A. Tranquilizers.
B. Sleeping pills.
B. Expectorants.
G. + Antihistamines.
97. Antihistamines:
1. Butadion.
2. Naphthyzin.
3. Tavegil.
4. Dimedrol.
A. True 2.3.
B. True 1.3.
B. + True 3.4.
G. True 2.4.
98. Antihistamine, not CNS depressant:
A. Dimedrol.
B. + Claritin.
V. Diprazine.
G. Suprastin.
99. Antiallergic agent used in bronchial asthma:
A. Adrenaline.
B. + Intal.
V. Naphthyzin.
G. Biseptol.
100. A drug used only to prevent attacks of bronchial asthma:
A. Alupent.
B. Berodual.
V. + Intal.
G. Berotek.
101. Asthmopent analogue:
A. + Berotek.
B. Anaprilin.
B. Hypothiazid.
G. Wisken.
102. Means effective for bronchial asthma:
1. Eufillin.
2. Codeine.
3. Asthmopent.
A. True 2.4.
B. True 1.2.
B. True 3.4.
D. + True 1.3.
103. Drugs used in bronchial asthma:
1. Whisken.
2. Berotek.
3. Atrovent.
4. Ketotifen.
A. + True 2,3,4.
B. True 1,2,3.
B. True 1.3.
G. True 2.4.
104. Effective in bronchial asthma:
3. Atrovent.
4. Atenolol.
A. True 2,3,4.
B. + True 1.3.
B. True 1.4.
G. True 1,2,3.
105. Bromhexine analogue:
A. Berotek.
B. Galazolin.
B. Hypothiazid.
G. + ACC (acetylcysteine).
106. Expectorant (mucolytic) agent:
A. Kodterpin.
B. + Solvin (Lazolvan).
V. Glauvent (Glaucin hydrochloride).
G. Libeksin.
107. Expectorants:
1. Bromhexine.
2. Ammonia-anise drops.
3. Alupent.
4. Allohol.
A. True 1.4.
B. True 3.4.
B. + True 1.2.
G. True 2.3.
108. Side effect of codeine:
A. + Drug addiction.
B. Cumulation.
B. Ototoxicity.
D. Teratogenicity.
109. Antitussives:
1. Sodium bicarbonate.
2. Ammonia-anise drops.
3. Codeine.
4. Libeksin.
A. + True 3.4.
B. True 1,2,3.
B. True 2.3.
G. True 1.3.
110. Antitussive:
A. Mukaltin.
B. Pektusin.
V. + Libeksin.
G. Terpinhydrate.
111. Expectorant:
A. Libeksin.
B. Tusuprex.
V. Glauvent.
G. + Lazolvan.
112. Drugs that suppress the cough center:
A. Terpinhydrate, libexin, omnopon.
B. Libexin, Bromhexine, Codeine, Omnopon.
B. + Oxeladin, libexin, codeine.
D. Terpinhydrate, oxeladin, libexin, bromhexine, codeine.
113. Pharmacological group of clonidine:
A. Antihistamines.
B. Antiarrhythmic drugs.
B. + Antihypertensive drugs.
D. Antianginal agents.
114. Analogue of anaprilin:
A. Berotek.
B. Oktadin.
B. Hypothiazid.
G. + Metoprolol.
115. For treatment hypertension apply:
A. + Captopril.
B. Digoxin.
B. Nitroglycerin.
G. Nitrong.
116. Validol is administered:
A. Orally.
B. Rectally.
B. + Sublingual.
G. Subarachnoid.
117. When cardiac arrest is administered intracardiac:
A. Atenolol.
B. + Adrenaline.
V. Anaprilin.
G. Mezaton.
118. Possible complication in the use of reserpine:
A. + CNS depression.
B. Allergy.
B. Excitation of the central nervous system.
G. Ototoxic effect.
119. A preparation containing the amount of rauwolfia alkaloids:
A. Aminazin.
B. Anaprilin.
V. + Adelfan.
G. Novopassit.
120. The cumulation of which drug is the most pronounced?
A. + Digitoxin.
B. Strofantin-K.
V. Adonizide.
G. Lily of the valley tincture.
121. Drug used in chronic heart failure:
A. + Celanid.
B. Korglikon.
B. Atropine sulfate.
G. Strofantin-K.
122. Validol:
B. Increases mental and physical performance, eliminates fatigue.
B. It has a vasoconstrictor and bronchodilatory effect, excites the central nervous system.
G. Inhibits the synthesis of folic acid, causes kidney crystalluria.
123. Analogue of nifedipine:
A. Klofelin.
B. Nitrogranulong.
V. Eufillin.
G. + Verapamil (Isoptin).
124. Antiarrhythmic drugs:
1. Amiodarone (cordarone).
2. Verapamil (Isoptin).
3. Reserpine.
4. Nitroglycerin.
A. True 1.3.
B. True 3.4.
B. + True 1.2.
G. True 2.4.
125. medicinal plants containing cardiac glycosides:
1. Lily of the valley.
2. Beauty.
3. Foxglove.
4. Adonis.
A. True 1.2.
B. + True 1,3,4.
B. True 1,2,4.
G. True 3.4.
126. Side effects arising from the use of nitroglycerin:
1. Dizziness, headache.
2. Increased blood pressure.
3. Redness of the skin of the face.
4. Lowering blood pressure.
A. True 1,2,4.
B. + True 1,3,4.
B. True 3.4.
G. True 2.4.
127. Nitroglycerin:
A. + It has a central, direct and reflex coronary dilating effect.
B. Increases mental and physical performance, eliminates fatigue.
B. It has a vasoconstrictor and bronchodilatory effect, excites the central nervous system.
G. It has an antirheumatic, analgesic effect.
128. For cupping hypertensive crisis apply:
1. Adelfan.
2. Pyrilene.
3. Benzohexonium.
4. Tincture of motherwort.
A. True 1.2.
B. + True 2.3.
B. True 3.4.
G. True 2.4.
129. The following drugs are used in chronic heart failure:
1. Digitoxin.
2. Digoxin.
3. Celanide.
4. Korglikon.
A. True 1.2.
B. + True 1,2,3.
B. True 2.3.
G. True 2,3,4.
130. Drugs acting on the renin-angiotensin system:
A. Labetalol, nifedipine, verapamil, dibazol.
B. + Enap, captopril.
B. Verapamil, dibazol.
G. Labetalol, Enap, nifedipine, captopril, verapamil, dibazol.
131. With repeated administration of digitoxin, the following may develop:
A. + Cumulation.
B. Synergism.
B. Habituation.
D. Drug addiction.
132. Angiotensin-converting enzyme inhibitor:
A. + Enalapril.
B. Atenolol.
B. Metoprolol.
G. Wisken.
133. In violation of cerebral circulation, apply:
A. Nitrong.
V. + Cavinton.
G. Lipostabil.
134. Digitalis preparation:
A. Korglikon.
B. + Celanid.
V. Adonizide.
G. Strofantin K.
135. Pharmacological group of nifedipine:
A. Beta-blockers.
B. Alpha-blockers.
B. + Calcium channel blockers.
G. Cardiac glycosides.
136. Antagonist of calcium ions:
A. Panangin.
B. Asparkam.
B. Novocainamide.
G. + Verapamil (Isoptin).
137. Antihypertensive drug that depresses the vasomotor center of the medulla oblongata:
A. + Clonidine.
B. Triresid.
V. Adelfan.
G. Furosemide.
138. Antihypertensive drug, AT-receptor blocker:
A. Corinfar.
B. + Kozaar.
V. Vinkapan.
G. Capoten.
139. Side effect of clonidine:
A. Hepatotoxic effect.
B. Nephrotoxic effect.
B. + Lethargy, drowsiness, dry mouth.
G. Tachycardia.
140. Prolonged form of nitroglycerin:
A. Erinit.
B. + Nitrogranulong.
V. Kordafen.
G. No-shpa.
141. Prolonged preparations of nitroglycerin:
A. Nitrolingval, nitrong, chimes.
B. + Nitrogranulong, trinitrolong, sustak, nitrong.
B. Trinitrolong, sustak, nitrong, chimes.
G. Nitrolingval, nitrogranulong, trinitrolong, sustak, nitrong, chimes.
142. Complications in the use of cardiac glycosides:
A. Hypotension, bronchospasm, increased intraocular pressure.
B. Dyspeptic symptoms, bronchospasm, increased intraocular pressure.
B. + Arrhythmia, dyspeptic phenomena.
G. Arrhythmia, dyspepsia, hypotension, bronchospasm, increased intraocular pressure.
143. Another name for nifedipine:
A. Dopegit.
B. Aldomet.
V. Lasix.
G. + Corinfar.
144. Another name for chimes:
A. Isoptin.
B. Methyldopa.
W. Nitrong.
G. + Dipyridamole.
145. Complex preparation potassium and magnesium for complex therapy IHD:
A. Verapamil.
B. Curantil.
V. No-shpa.
G. + Panangin.
146. Drugs used to stop angina attacks:
1. Sustak.
2. Nitroglycerin.
3. Validol.
4. Dibazol.
A. True 1.2.
B. True 2.4.
B. True 1,2,4.
D. + True 2.3.
147. Pharmacological properties validola:
1. Leads to reflex expansion
coronary vessels.
2. Irritates the receptors of the oral cavity.
3. Has an antispasmodic effect.
A. True 1.3.
B. + True 1.2.
B. True 2.3.
148. Medications used to treat hypertension:
1. Adrenaline.
3. Atropine.
4. Atenolol.
A. True 1.2.
B. + True 2.4.
B. True 2,3,4.
G. True 1.3.
149. The following preparations are used in acute heart failure:
1. Korglikon.
2. Adonizide.
3. Lily of the valley tincture.
4. Strofantin-K.
A. True 2.3.
B. True 1.3.
B. True 2.4.
D. + True 1.4.
150. Drugs used to prevent angina attacks:
1. Sustak.
2. Nitrosorbide.
3. Validol.
4. Nitrong.
A. + True 1,2,4.
B. True 2,3,4.
B. True 1.2.
G. True 2.4.
151. Antihypertensive drugs central action:
1. Adrenaline hydrochloride.
2. Clonidine.
3. Dopegyt.
4. Papaverine hydrochloride.
A. True 1.2.
B. + True 2.3.
B. True 3.4.
G. True 2.4.
152. For the treatment of atherosclerosis use:
1. Nifedipine.
2. Lovastatin.
3. Cholestyramine.
4. Enalapril.
A. True 1,2,3.
B. + True 2.3.
B. True 2,3,4.
G. True 1.2.
153. Means that improve cerebral circulation:
1. Nifedipine.
2. Cinnarizine.
4. Vinpocetine.
A. True 1,2,3.
B. + True 2.4.
B. True 3.4.
G. True 1.4.
154. Cardiac glycosides are used for:
A. Hypertension.
B. + Heart failure.
B. Atherosclerosis.
G. Angina pectoris.
155. For promotion blood pressure use:
A. Xylometazoline.
B. + Mezaton.
B. Benzohexonium.
G. Reserpine.
156. To antihypertensive drugs - ACE inhibitors applies to:
A. Verapamil.
B. Reserpine.
B. + Enalapril.
G. Dibazol.
157. Antiarrhythmic drugs include:
1. Clonidine.
2. Quinidine.
3. Aymalin.
4. Novocainamide.
A. True 1,2,3.
B. Correct 1,3,4.
B. + True 2,3,4.
G. True 1,2,4.
158. Hypotensive activity is possessed by:
1. Arifon.
2. Corinfar.
4. Enalapril.
A. True 1,2,3.
B. + True 1,2,4.
B. True 3.4.
G. True 1.2.
159. The group of calcium ion antagonists includes:
1. Vinpocetine.
2. Nifedipine.
3. Verapamil.
4. Diltiazem.
A. True 1.3.
B. True 2.3.
B. True 3.4.
D. + True 2,3,4.
160. Cardiac glycoside used in heart neuroses:
A. Digitoxin.
B. + Tincture of lily of the valley.
V. Strofantin-K.
G. Korglikon.
161. Mevacor:
A. + Lowers blood cholesterol levels.
B. Expands the vessels of the brain.
B. Reduces the heart's need for oxygen.
G. Reduces the heart rate.
162. In case of acute heart failure, the following is prescribed:
A. Digitoxin.
B. + Korglikon.
V. Adonizide.
G. Adonis bromine.
163. The drug used to stop angina attacks:
A. + Nitroglycerin.
B. Sustak.
W. Nitrong.
G. Nitroderm.
164. Triampur is applied:
B. With chronic constipation.
B. + With edema of cardiac and renal origin.
G. With infections of the respiratory tract, genitourinary tract, infections of the gastrointestinal tract.
165. Combined diuretic drugs:
A. Lasix, triampur, uregit.
B. + Triampur, amyloretic.
B. Oxodoline, amyloretic, uregit, clopamid.
G. Lasix, triampur, uregit, oxodoline, amyloretic, clopamid.
166. Potassium-sparing diuretic:
A. Hypothiazide.
B. Furosemide.
V. Diacarb.
G. + Veroshpiron.
167. Diuretics:
1. Hypothiazid.
2. Furosemide.
3. Spironolactone.
4. Magnesium sulfate.
A. True 1.2.
B. True 2,3,4.
B. + True 1,2,3.
G. True 3.4.
168. Another name for veroshpiron:
A. Lasix.
B. Triampur.
B. + Spironolactone.
G. Hypothiazid.
169. Thiazide diuretics:
1. Furosemide.
2. Chlortalidone.
3. Veroshpiron.
4. Hypothiazide.
A. True 1.4.
B. Everything is true.
B. True 1,2,4.
D. + True 2.4.
170. Diuretics include:
1. Fentanyl.
2. Furosemide.
3. Captopril.
4. Hypothiazide.
A. True 1.2.
B. True 1,2,3.
B. + True 2.4.
G. True 2,3,4.
171. Osmotic diuretic:
A. Hypothiazide.
B. + Mannitol.
B. Furosemide.
G. Triampur.
172. Another name for uregit:
A. Triamteren.
B. Lasix.
B. Hypothiazid.
D. + Ethacrynic acid.
173. Diuretic - aldosterone hormone antagonist:
A. Furosemide.
B. + Veroshpiron.
V. Oxodolin.
G. Cyclomethiazide.
174. By-effect hypothiazide:
A. Carcinogenicity.
B. + Hypokalemia.
B. Collapse.
G. Withdrawal syndrome.
175. Another name for indapamide:
A. Dichlothiazide.
B. Diacarb.
V. Uregit.
G. + Arifon.
176. Drug used as cholagogue:
A. Bisacodyl.
B. + Allohol.
V. Biseptol.
G. Venter.
177. Karsil is applied:
A. + As a hepatoprotective agent.
B. With indomitable vomiting.
B. For constipation.
G. When hyperacidity stomach.
178. Drugs used for acute constipation:
1. Kafiol.
2. Magnesium sulfate. .
3. Sodium sulfate.
4. Laminaria.
A. True 1.2.
B. True 3.4.
B. + True 2.3.
G. True 1.4.
179. Drugs used for treatment peptic ulcer stomach:
1. Famotidine.
2. Almagel A.
4. Thermopsis.
A. + True 1,2,3.
B. True 1.3.
B. True 2,3,4.
G. True 2.4.
180. Pancreatin is used:
A. With rheumatoid arthritis, inflammation of the joints.
B. With chronic constipation.
B. With edema of cardiac and renal origin.
G. + In chronic pancreatitis.
181. Pharmacological group Essentiale:
A. Laxatives.
B. Antacids.
B. Diuretics.
G. + Hepatoprotectors.
182. Analogue of festal:
A. + Mezim-forte.
B. Gastal.
B. Bifidumbacterin.
G. Ranitidine.
183. Features of the use of pancreatin powder:
1. Inside, before eating.
2. Inside, after eating.
3. Drink alkaline water.
4. Rectally.
A. + True 1.3.
B. True 2,3,4.
B. True 2.4.
G. True 2.3.
184. Drugs used in hypoacid gastritis:
1. Pepsin.
2. Sodium bicarbonate.
3. Hydrochloric acid.
4. Almagel.
A. True 1.2.
B. True 2.3.
B. + True 1.3.
G. True 3.4.
185. Antacids:
1. Plantaglucid.
2. Maalox.
3. Almagel.
4. Gastrocepin.
A. True 1.2.
B. + True 2.3.
B. True 3.4.
G. True 1.4.
186. Preparations that promote bile formation:
1. Holosas.
2. Allohol.
3. Essentiale.
4. Flamin.
A. True 1,2,3.
B. + True 1,2,4.
B. True 1.2.
G. True 3.4.
187. Cholagogue drug from the group of choleretics of synthetic origin:
A. Holenzim.
B. Holosas.
B. + Oxaphenamide.
G. Flamin.
188. M-holinoblokator for the treatment of gastric ulcer:
A. + Gastrocepin.
B. Imodium.
B. Sucralfat.
G. Ranitidine.
189. Choleretic drug obtained from the flowers of common tansy:
A. + Tanacehol.
B. Holosas.
V. Allohol.
G. Holenzim.
190. Antacid:
A. + Gastal.
B. Ranitidine.
B. Cimetidine.
G. Acidine-pepsin.
191. Bismuth drug with gastroprotective action:
A. Phosphalugel.
B. Smekta.
V. + De-Nol.
G. Almagel.
192. Blockers H 2 -histamine receptors:
A. + Cimetidine, ranitidine, famotidine.
B. Ranitidine, famotidine, pirenzepine.
B. Famotidine, cimetidine, pirenzepine.
D. Cimetidine, ranitidine, famotidine, pirenzepine.
193. Chronic pancreatitis is treated with:
A. Fibrinolysin.
B. Contrykal.
W. Gordox.
G. + Festal.
194. For the treatment of gastric ulcer apply:
A. Gastric juice.
B. Abomin.
B. + Omeprazole.
G. Pancreatin.
195. Phosphalugel analogue:
A. Abomin.
B. Allohol.
B. Ambroxol.
G. + Maalox.
196. Means used for chronic constipation:
1. Festal.
2. Bisacodyl.
3. Magnesium sulfate.
4. Antrasennin.
A. True 1.3.
B. + True 2.4.
B. True 1.2.
Option number 1
What does the term "pharmacodynamics" include?
1. Absorption of medicinal substances. 2. Distribution of medicinal substances in the body. 3. Deposition of medicinal substances. 4. Localization of the action of medicinal substances. 5. Mechanisms of action. 6. Pharmacological effects. 7. Types of action. 8. Biotransformation. 9. Removal of drugs from the body.
What is the accumulation of drugs in the body during repeated administration called?
1. Functional cumulation. 2. Material cumulation. 3. Sensitization.
With repeated use of drugs, there may be:
1. Antagonism; 2. Addictive; 3. Cumulation; 4. Tachyphylaxis; 5. Drug addiction.
Task.
WHAT FEATURES (A-B) CORRESPOND TO THE PROPERTIES OF THE FULL AGONIST, PARTIAL AGONIST AND ANTAGONIST?
|
Property Substance |
Affinity |
Internal Activity |
Influence of factors of the internal and external environment on the action of medicinal substances. Reactions of the body to repeated and combined action of drugs.
Option number 2
Answer the test control questions, indicate one or more correct answers:
Mark 4 main "targets" for drugs:
1. Specific receptors. 2. Structural proteins. 3. Transport systems. 4. Ion channels. 5. Enzymes.
What is characteristic of addiction to a drug when it is repeated?
1. An irresistible desire for a constant intake of a medicinal substance. 2. Strengthening the effect of the medicinal substance. 3. Weakening of the effect of the medicinal substance. 4. Abstinence upon drug withdrawal.
The term "pharmacodynamics" includes:
1. Mechanism of action; 2. Types of action; 3. Biotransformation medicines; 4. Localization of action; 5. Pharmacological effects.
Task.
WHAT SUBSTANCE (AB) IS A FULL AGONIST, PARTIAL AGONIST, ANTAGONIST?
Influence of factors of the internal and external environment on the action of medicinal substances. Reactions of the body to repeated and combined action of drugs.
Option number 3
Answer the test control questions, indicate one or more correct answers:
Affinity:
What characterizes physical drug dependence?
1. An irresistible desire for a constant intake of a medicinal substance. 2. Improvement in well-being after taking the drug. 3. The possibility of rapid withdrawal of the drug in the treatment of drug dependence. 4. The need to gradually reduce the dose of the drug in the treatment of drug dependence. 5. Abstinence.
With the combined administration of drugs, the following can be observed:
1. Additive effect; 2. Antagonism; 3. Addictive; 4. Potentiation.
Task.
WHAT IS THE CHARACTER OF THE INTERACTION OF SUBSTANCE A AND B IN THEIR COMBINED APPLICATION (A+B)?
Average values with confidence limits are given.
Influence of factors of the internal and external environment on the action of medicinal substances. Reactions of the body to repeated and combined action of drugs.
Option number 4
Answer the test control questions, indicate one or more correct answers:
Internal activity:
1. The ability of a substance to bind to specific receptors. 2. The ability of a substance to cause an effect when interacting with receptors. 3. The amount of dose at which the substance causes the maximum effect.
What is the term for unusual drug reactions?
1. Sensitization. 2. Tachyphylaxis. 3. Idiosyncrasy.
Medicines are combined with the aim of:
1. Reducing the manifestation of the negative effects of drugs; 2. Increasing the therapeutic effect; 3. Increasing the therapeutic concentration of one of the drugs in the blood; 4. Accelerating the excretion of one of the drugs from the body.
Task.
WHAT IS THE OBSERVED INTERACTION OF TWO DRUGS NAMED?
Registration of changes in the amplitude of contractions of the gastrocnemius muscle during electrical stimulation of the motor nerve. 1 - after the introduction of pipecuronium, 2 - against the background of inhalation of ether and subsequent administration of pipecuronium.
Influence of factors of the internal and external environment on the action of medicinal substances. Reactions of the body to repeated and combined action of drugs.
After the drug enters the systemic circulation, it is distributed to the tissues of the body. Distribution is usually uneven due to differences in hemoperfusion, tissue binding (eg, different fat content), local pH, and cell membrane permeability.
The rate of penetration of the drug into the tissue depends on the rate of blood flow in the tissue, the size of the tissue and the characteristics of the distribution between blood and tissue. The balance of distribution (when the rates of penetration and elimination from the tissue are the same) between blood and tissue is more quickly achieved in areas of rich vascularity, if diffusion through the cell membrane is not a rate limiting factor. After equilibrium is reached, drug concentrations in tissue and extracellular fluids are proportional to plasma concentrations. Metabolism and elimination occur simultaneously with distribution, making the process dynamic and complex.
For the interstitial fluids of most tissues, the rate of drug distribution is determined primarily by perfusion. Tissues that are poorly perfused (eg, muscle, fat) are characterized by very slow distribution, especially if the tissue has a high affinity for the drug.
Volume of distribution
The apparent volume of distribution is the estimated volume of fluid in which the total amount of drug administered is distributed to create a concentration corresponding to that in plasma. For example, if 1000 mg of a drug is administered and the plasma concentration is 10 mg/L, then 1000 mg is distributed in 100 L (dose/volume=concentration; 1000 mg/L=10 mg/L; hence: =1000 mg/10 mg/l=100 l). The volume of distribution has nothing to do with body volume or fluid content, but rather depends on the distribution of the drug in the body. For drugs that easily cross tissue barriers, a relatively small dose remains in the circulation and thus the plasma concentration will be low and the volume of distribution high. Drugs that preferentially remain in the circulatory system often have a low volume of distribution. The volume of distribution characterizes the concentration in blood plasma, but gives little information about the specific mode of distribution. Each drug is unique in its distribution in the body. Some get mainly into fats, others remain in the extracellular fluid, and others are distributed into tissues.
Many drugs that are acidic (for example, warfarin, salicylic acid) binds well to proteins and thus has a low apparent volume of distribution. Many bases (eg, amphetamine, pethidine), on the other hand, are extensively taken up by tissues and thus have an apparent volume of distribution greater than that of the whole body.
Binding
How a drug is distributed to tissues depends on its binding to plasma and tissue proteins. In the bloodstream, drugs are partially transported in solution as a free (unbound) fraction, and partially as a bound fraction (for example, with plasma proteins or blood cells). Of the numerous plasma proteins that can interact with the drug, the most important are albumin, acid glycoprotein and lipoproteins. Drugs whose solutions are acidic usually bind more strongly to albumin. Bases, on the contrary, are with acidic glycoprotein and/or lipoproteins.
Only an unbound drug is capable of passive diffusion into extravascular spaces or tissues where it is administered. pharmachologic effect. Therefore, the concentration of unbound drug in big circle blood circulation usually determines its concentration at the site of the effect and, thus, the severity of the latter.
At high concentrations, the amount of bound drug reaches a maximum, determined by the amount available seats for binding. Saturation of binding sites is the basis of the displacement effect in drug interactions.
Drugs are able to bind to various substances, not only proteins. Binding usually occurs when the drug interacts with the macromolecule in a liquid medium, but can also occur when it enters the adipose tissue of the body. Since fat is poorly perfused, the time to reach equilibrium is usually long, especially if the drug is highly lipophilic.
The accumulation of drugs in tissues or areas of the body can prolong their effect, as the tissues release the accumulated drug as the plasma concentration decreases. For example, thiopental has a significant solubility in fats, quickly penetrates into the brain after a single intravenous injection and is characterized by the development of a pronounced and rapid anesthetic effect; it then wears off within minutes as it redistributes into slowly perfused adipose tissue. Thereafter, thiopental is slowly released from adipose tissue, maintaining subanesthetic plasma concentrations. However, with repeated administration, these concentrations can become significant, causing the drug to in large numbers accumulate in adipose tissue. Thus, this process first reduces the effect of the drug, but then prolongs it.
Some drugs accumulate in cells due to binding to proteins, phospholipids, or nucleic acids. For example, the concentration of chloroquine in leukocytes and hepatocytes can be a thousand times higher than in blood plasma. The drug in the cells is in equilibrium with its concentration in the blood plasma and passes there as the plasma fraction is eliminated from the body.
Blood-brain barrier
Drugs reach the CNS through the capillaries of the brain and cerebrospinal fluid. Although the brain receives about a sixth cardiac output, the distribution of drugs into the brain tissue is limited because the permeability of the brain differs from that of other tissues. Some fat-soluble drugs (eg, thiopental) easily enter the brain, but this is not the case for polar compounds. The reason for this is the blood-brain barrier, which consists of the endothelium of the capillaries of the brain and the astrocytic-glial membrane. The endothelial cells of the capillaries of the brain, which appear to be more closely connected to each other than the cells of most capillaries, slow down the diffusion of water-soluble drugs. The astrocytic-glial sheath consists of a layer of glial cells connective tissue(astrocytes) located near the basement membrane of the capillary endothelium. With age, the blood-brain barrier may become less effective, leading to increased penetration of various substances into the brain.
Medicines may enter cerebrospinal fluid ventricles directly through the choroid plexus, then passively diffuse into the brain tissue from the cerebrospinal fluid. in the choroid plexus organic acids(for example, benzylpenicillin) are actively transferred from the cerebrospinal fluid into the blood.
With regard to cells of other tissues, the rate of penetration of the drug into the cerebrospinal fluid is mainly determined by the degree of protein binding, the degree of ionization and the solubility of the drug in fats and water. The rate of penetration into the brain is slow for drugs that are largely associated with proteins, and quite insignificant for ionized forms of weak acids and bases. Since the CNS is well supplied with blood, the rate of drug distribution is determined primarily by permeability.
Metabolism
The liver is the main organ where drug metabolism occurs. Although metabolism usually leads to inactivation of drugs, some of their metabolites are pharmacologically active, sometimes even more active than the parent compound. An parent substance that has no pharmacological activity or weak pharmacological activity, but has active metabolites, is called a prodrug, especially if it is intended to provide more complete delivery.
Drugs can be metabolized by:
oxidation;
recovery;
hydrolysis;
hydration;
conjugation;
condensation or isomerization.
However, whatever the process, its purpose is to facilitate the process of elimination. Enzymes involved in metabolism are present in many tissues, but at the same time are predominantly concentrated in the liver. The rate of drug metabolism is individual. Some patients metabolize drugs so rapidly that therapeutically effective blood and tissue concentrations are not reached. In other patients, the metabolism may be so slow that the usual doses are toxic. metabolic rate individual drugs depends on genetic factors, the presence of concomitant diseases (especially chronic diseases liver and decompensated heart failure) and drug interaction(especially involving the induction or inhibition of metabolism).
The metabolism of many drugs occurs in two phases:
The reactions of the first phase include the formation of new or modification of existing functional groups, or the splitting of the molecule (by oxidation, reduction, hydrolysis). These reactions are not synthetic.
Second phase reactions involve conjugation with endogenous substances (eg glucuronic acid, sulfate, glycine) and are synthetic.
Metabolites formed as a result of synthetic reactions are more polar and more easily excreted by the kidneys (with urine) and liver (with bile) than metabolites formed by non-synthetic reactions. Some drugs undergo only the first or only the second phase reactions. Thus, the number of phases reflects a functional rather than a sequential classification.
Speed
For almost all drugs, the rate of metabolism by any pathway has an upper saturation limit. However, at therapeutic concentrations, most drugs take up only a small fraction of the potential of the metabolizing enzyme, and the rate of metabolism increases as drug concentration increases. In such cases, described as first-order elimination (or kinetics), the rate of drug metabolism is a constant fraction of the drug remaining in the body (rather than a constant amount of drug per hour), i.e. the drug has a certain half-life. For example, if 500 mg of the drug is present in the body at zero point, 250 mg remains in metabolism after 1 hour, 125 mg after 2 hours (corresponding to a half-life of 1 hour). However, when most enzyme binding sites are occupied, metabolism occurs with maximum speed and does not depend on the concentration of the drug in the blood, i.e., a fixed amount of the drug is metabolized per unit time, which is described by the term "zero order kinetics". In this case, if 500 mg of the drug is present in the body at the zero point, then after 1 hour 450 mg may remain as a result of metabolism, after 2 hours - 400 mg (which corresponds to a maximum clearance of 50 mg / h in the absence of a certain half-life value). As the concentration of the drug in the blood increases, the metabolism, which was originally described by first-order kinetics, begins to correspond to zero-order kinetics.
Cytochrome P450
The most important enzymatic system of the first phase metabolism, cytochrome P450, is a family of microsomal isoenzymes that catalyze the oxidation of many drugs. The electrons necessary for this are provided by NADP H (with the participation of cytochrome P450 reductase, a flavoprotein that transfers electrons from NADP H, which is a reduced form of nicotinamide adenine dinucleotide phosphate, to cytochrome P450). Isoenzymes of the cytochrome P450 family can be induced and inhibited by many drugs and substances, thus being the cause of the interaction of many drugs, when one of them increases toxicity or reduces therapeutic effect another.
With age, the ability of the liver to metabolize by cytochrome P450 decreases by 30% or more, as the volume of the liver and the activity of blood flow in it decrease. Thus, in the elderly, drugs metabolized by these enzymes are characterized by more high values concentration and half-life. At the same time, since newborns have an underdeveloped system of microsomal liver enzymes, they hardly metabolize many drugs.
Conjugation
Glucuronidation is the most common second phase reaction and the only reaction occurring in microsomal liver enzymes. Glucuronides are secreted in the bile and excreted in the urine. Thus, conjugation makes most drugs more soluble, making them easier to excrete by the kidneys. As a result of the conjugation of amino acids with glutamine or glycine, products are formed that are easily excreted in the urine and secreted only in small amounts in the bile. The intensity of glucuronidation does not depend on age, however, in newborns, the process of glucuronide formation is slower, which in some cases can cause serious undesirable effects.
Conjugation via acetylation and sulfonic conjugation is also possible. Sulfated esters are polar and are easily excreted in the urine. The intensity of these processes does not depend on age.
Excretion
The kidneys excrete water-soluble substances and are the main organs of excretion. The biliary system also facilitates the elimination of drugs, provided that they are not reabsorbed in the gastrointestinal tract. Usually the role of intestines, saliva, sweat, breast milk and lungs in excretion is small, except for the excretion of volatile drugs for anesthesia. Withdrawal from breast milk, although not affecting the mother, may have an effect on the breastfed infant.
Metabolism in the liver often makes drugs more polar and thus more water soluble. Metabolites resulting from this process are more easily excreted from the body.
renal excretion
Most drugs are excreted by renal filtration. About 20% of the blood plasma entering the glomerulus is filtered by its endothelium, then almost all water and most electrolytes are passively or actively reabsorbed from the renal tubules back into the bloodstream.
However, polar compounds, which include most drug metabolites, cannot diffuse back into the bloodstream (in the absence of a specific transport mechanism for their reabsorption, for example, as in the case of glucose, ascorbic acid and vitamins of group B) and are excreted from the body. With age, the excretion of the drug by the kidneys decreases. At the age of 80 years, the clearance value usually corresponds to 50% of the same value at the age of 30 years.
Pathways for the transport of drugs in the kidneys are directly related to the mechanisms of transmembrane transport. Drugs bound to plasma proteins remain in the bloodstream. As a result, only the unbound portion of the drug is contained in the glomerular filtrate. Non-ionized forms of drugs and their metabolites tend to be easily reabsorbed from the lumen of the tubules.
Urinary pH, ranging from 4.5 to 8.0, can also have a marked effect on drug reabsorption and excretion by determining whether a weak acid or base is in a non-ionized or ionized form. Acidification of the urine increases reabsorption and reduces the excretion of weak acids and reduces the reabsorption of weak bases. Alkalinization of urine has the opposite effect. In some cases of overdose, these principles are used to enhance the excretion of weak bases or acids, for example, the urine is alkalized to enhance excretion. acetylsalicylic acid. The extent to which a change in urine pH affects the rate of drug excretion depends on the degree of participation of the kidneys in the overall elimination of the drug, on the polarity of the non-ionized form and the degree of ionization of the molecule.
Active secretion in the proximal tubules great importance in the elimination of many drugs. This energy-dependent process can be blocked by metabolic inhibitors. At high drug concentrations, secretory transport can reach a higher limit (transport maximum). Each substance has a characteristic transport maximum.
The transport of anions and cations is controlled by special mechanisms. Usually, the anionic secretory system removes metabolites conjugated with glycine, sulfate, or glucuronic acid. In this case, anions (weak acids) compete with each other for excretion, which can be used for therapeutic purposes. For example, probenecid generally blocks the rapid tubular secretion of benzylpenicillin, resulting in a higher plasma concentration of the latter over a longer period of time. In the cation transport system, cations or organic bases (eg, pramipexole, dofegilide) are secreted by the renal tubules. This process can be inhibited by cimetidine, trimethoprim, prochlorperazine, megestrol or ketoconazole.
Excretion with bile
Some drugs and their metabolites are actively excreted in the bile. Since they are transported through the epithelium biliary tract against the concentration gradient, the presence of active transport mechanisms is required. At a high concentration of the drug in the blood plasma, secretory transport may approach the highest limit (transport maximum). Substances with similar physical and chemical properties can compete for excretion.
medicines with molar mass greater than 300 g/mol and having polar and lipophilic groups are likely to be excreted in the bile. Smaller molecules are usually excreted in this way only in small amounts. Conjugation with glucuronic acid facilitates biliary excretion.
In the enterohepatic circulation, the drug secreted in the bile is reabsorbed into the bloodstream from the intestine. Bile excretion removes substances from the body only when the enterohepatic cycle becomes incomplete, i.e. when a certain part of the secreted drug is not reabsorbed from the intestine.
Pharmacodynamics
Pharmacodynamics is sometimes understood as the effect a drug has on the body, including receptor binding (including receptor sensitivity), post-receptor effects, and chemical interactions. Pharmacodynamics together with pharmacokinetics (the influence of the body on the drug) allows us to explain the effects of the drug.
The pharmacodynamics of a drug may be affected by changes that occur as a result of disturbances in the body, aging, or the effects of other drugs. Conditions that affect the pharmacodynamic response include mutations, thyrotoxicosis, malnutrition, myasthenia gravis, and some forms of non-insulin dependent diabetes mellitus.
These conditions can affect receptor binding, alter the concentration of binding proteins, or desensitize receptors. With age, a change in the pharmacodynamic response is also possible, which is due to changes in the connection with receptors or post-receptor effects. Pharmacodynamic drug interactions result in competition for receptor binding or altered post-receptor response.