PHARMACEUTICAL FORMS AND DOSES

Antibiotics of a wide spectrum,

Antituberculous agents

1. Determine the group of the drugs:

chloramphenicol, amikacin, tetracycline, gentamicin, clindamycin, vancomycin, polymyxin M, doxycycline, tobramycin, sisomycin, lincomycin, teicoplanin.

 

Tetracyclines (2); gr. levomycetin (1); aminoglycosides (4); glycopeptides (2); lincosamides (2); polymyxins (1).

 

2. Determine the mechanism of action and effect of drugs and fill in the table:

Name of the group	Type of action	Mechanism of action
Group of Levomycetin
Aminoglycosides
Tetracyclines
Glycopeptides
Polymyxins

1. Drugs change the configuration of the 30S subunit, which leads to incorrect reading of the mRNA code. They disrupt the initiation of protein synthesis, cause premature termination of translation and use of incorrect amino acids in the synthesis. As a result, abnormal proteins are synthesized. Drugs also violation of the permeability of the cytoplasmic membrane.

2. The drugs bind to the 30s ribosome subunit, blocking the attachment of aminoacyl-tRNA to the aminoacyl site of the ribosome-mRNA complex. As a result, drugs inhibit of protein synthesis.

3. The drug binds to the 50s subunit of the ribosome and inhibits peptidyltransferase (an enzyme that catalyzes the inclusion of amino acids in the growing polypeptide chain) in the peptide site. As a result, drugs inhibit of protein synthesis.

4. The drugs block the final stage of peptidoglycan synthesis. The antibiotic molecule binds to the terminal amino acids in the side peptide chain and blocks the cross-linking of peptidoglycan, thus disrupting the synthesis of the bacterial cell wall.

5. Drugs are cationic main polypeptides that attach to the bacterial cell membrane, disrupt its permeability and transport mechanisms, which lead to bacterial lysis.

 

3. Determine of Spectrum of Tetracyclines and Chloramphenicol:

	tetracyclines	chloramphenicol
a) act
b) do not work

Cocci, Haemophilus influenza, Neisseria, Escherichia coli, Shigella, Salmonella, Clostridia,Chlamydia, Rickettsia, pathogens of especially dangerous infections (cholera, plague, brucellosis, tularemia, anthrax), Pseudomonas aeruginosa, mycobacterium tuberculosis, fungi, viruses, Plasmodium falciparum.

4. Complete the statements:

Tetracyclines are contraindicated during pregnancy and for children less than 8 years old, because…

Chloramphenicol is contraindicated during pregnancy, because…

Tetracycline should not be taken together with dairy products and drugs calcium, because....

Doxycycline is not used to treat meningitis, because....

The use of broad-spectrum antibiotics is accompanied by the development of dysbiosis, because ....

Situational task

The dentist discovered a child with three years of multiple caries, a delay in the development of teeth, their deformation, yellowing. What antibiotic was the mother taking during pregnancy?

6. Determine the drugs (tetracycline, chloramphenicol, amikacin) according to pharmacokinetic parameters:

Parameter	А	B	C
Absorption from the digestive tract	Not absorbed	Very good	Good
Penetration in the central nervous system	Does not pass	Very good	The bad
Penetration into the focus of infection	Slow and incomplete	Fast and good	Good
Excretion	Primarily the kidneys are unchanged	Primarily, the kidneys in the form of inactive metabolites	Kidney and bile

7. Classify aminoglycosides (kanamycin, sisomycin, neomycin, amikacin, streptomycin, gentamicin, tobramycin) for generations:

Generation (3), 2 generation (1), 3 generation (3).

 

Identify kanamycin, gentamicin, amikacin

Range	А	B	C
Cocci	+	+	+
E. coli, Shigella, Salmonella	+	+	+
Pathogens of plague, tularemia, brucellosis	+	+	+
Mycobacteria	+	-	+
Pseudomonas aeruginosa	+	+	-

9. Identify tetracycline, chloramphenicol, streptomycin:

Complication	A	B	C
Syndrome of irritation of mucosa	+	-	+
Hepatotoxic effect	+	-	+
Ototoxic effect	-	+	-
Nephrotoxicity	-	+	-
Inhibition of hematopoiesis	+	-	±
Violation of neuromuscular conduction	-	+	-
Defect in the rudiment of teeth and bones	-	-	+

1 0 . Choose the correct answer:

Polymyxin M in the microbial cell disrupts (protein synthesis / permeability of the cytoplasmic membrane), acts (bacteriostatic / bactericidal) on (Gr + / Gr-flora), the resistance of microorganisms develops (fast / slow), appointed (inside and locally / parenterally only).

11. Classify anti-tuberculosis drugs:

Antibiotics

Synthetic drug

streptomycin, kanamycin, isoniazid, rifampicin, ethambutol, pyrazinamide, aminosalicylic acid.

 

12. Answer the questions:

Isoniazid and rifampicin are class A antituberculosis drugs, since ...

In the treatment of patients with tuberculosis, several drugs are prescribed simultaneously, since ...

Aminosalicylic acid enhances the action of isoniazid, since ...

It is advisable to administer isoniazid with vitamin B6, since ...

13. Determine anti-TB drugs ethambutol, isoniazid, kanamycin, rifampicin.

	Spectrum	Mechanism of action	Resistance	Side effects
А	Wide	Block of DNA-dependent RNA polymerase	Fast	Allergic reactions, hepatotoxicity, dysbacteriosis
B	Mycobacteria	Violation of the synthesis of mycolic acids, violation of cellular respiration.	Slow	Peripheral neuritis, convulsions, insomnia.
C	Wide	Violation of protein synthesis, violation of the permeability of the cytoplasmic membrane	Fast	Hearing loss, vestibular disorders, impaired renal function, allergic reactions.
D	Mycobacteria	Disturbance of the synthesis of RNA and proteins	Slow	Visual impairment, allergic reactions

 

Write the prescriptions

1. Drug for the treatment of meningococcal infection in tablets
2. An antibiotic for the treatment of conjunctivitis
3. Drug for the treatment of brucellosis (Lyme disease) in tablets
4. Drug for the treatment of pneumonia associate with Pseudomonas aeruginosa in ampoules.
5. The drug from the group of lincosamide, oppresses the synthesis of protein, acts bacteriologically on anaerobes, cocci. Well penetrates into bone tissue. It is prescribed for infections of the abdominal cavity, ENT organs, with diseases of bones, joints. It is used orally, parenterally, topically. May cause pseudomembranous colitis.
6. It is a first-line anti-tuberculosis drug, block of DNA-dependent RNA polymerase, it is also used to treat leprosy and to prevent meningococcal meningitis in people who have been in close contact with the diseased.

 

PHARMACEUTICAL FORMS AND DOSES

INN	Drug form s	Method of application
Tetracyclin е	100 mg tablets	1-2 tablets 4 times a day after meals
	1% eye ointment 10 grams	Lay behind the lower eyelid 3-5 times a day
	3% ointment 15 grams	Apply on the affected skin 1-2 times a day
Doxycycline	100 mg tablets (capsules)	The first day 1 capsules 2 times, next day’s 1 capsule once a day.
	100 and 200 mg in ampoules	Inject I.V. 200 mg in 200-400 ml of isotonic sodium chloride solution once a day
Chloramphenicol	250 and 500 mg tablets (capsules)	1-2 tablets (caps.) 3-4 times a day 30 minutes before meals
	0,25% solution in 10 ml vials	1 drop in both eyes 3 times a day
	1% alcohol solution in 25 ml vial	Apply on the affected skin 2-3 times a day
Gentamycin	Solution 40 mg/ml in 1 and 2 ml amp.	Inject I.M. 1-2 ml 2-3 times a day
	0,1% ointment 10 grams	Lubricate the affected skin 2-3 times a day
Tobramycin	Solution 40 mg/ml in 2 ml amp.	Inject I.M. 2 ml (I.V. drip in 50-100 ml of isotonic sodium chloride solution) 2-3 times a day
	0,3% solution in 5 ml vial	1-2 drops in both eyes 4-6 times a day
Sisomycin	Solution 50 mg/ml in 1 ml amp.	Inject I.M. 1-2 ml twice a day
	0,3% solution in 5 ml vial	1-2 drops in both eyes 4-6 times a day
Amikacin	Solution 250 mg/ml in 2 ml amp.	Inject I.M. 2 ml (I.V. drip in 200 ml of isotonic sodium chloride solution) 2 times a day
	500 and 1000 mg in 10 ml vials	Inject I.M. 500 (1000) mg twice a day
Vancomycin	500 and 1000 mg in vials	Inject I.V. drip 500 (1000) mg in 200 ml of isotonic sodium chloride solution 2-4 times a day
Clindamycin	150 and 300 mg capsules	1 capsule 4 times a day
	Solution 150 mg/ml in 2 ml amp.	Inject I.M. (I.V. slowly) 2 ml 2-3 times a day
	100 mg suppositories	Insert in vagina 1 suppository before bedtime
	1% gel 30 grams	Apply on the affected skin 2-3 times a day
	2% vaginal cream 20 grams	5 grams in the vagina with an applicator at night
Isoniazid	100; 200 and 300 mg tablets	1 tablet 1-3 times a day
	Sol. 100 mg/ml in 10 ml amp.	Inject I.M. (I.V. slowly) 5 ml once a day
Rifampicin	150; 300 and 600 mg capsules	1-2 capsules once a day before meals
Streptomycin	500 and 1000 mg in 10 ml vials	Inject I.M. 500 (1000) mg in 2-4 ml of water pro injections twice a day
Kanamycin	500 and 1000 mg in 10 ml vials	Inject I.M. 500 (1000) mg in 2-4 ml of water pro injections twice a day
Ethambutol	100; 200; 400 and 600 mg tablets	1 tablet once a day
Pyrazinamid е	250; 500 and 1000 mg tablets	1500-2000 mg once a day
Aminosalicylic acid	500 and 1000 mg tablets	3-6 tablets 3 times a day after meals

 

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