Written Pharmacology Flashcards
2 Adverse Effects of Penicllins:
Allergic Reactions: angioedema & Anaphylactic shock
CNS irritation (seizures) may occur with large doses in patients with renal failure
Discuss Toxicity of Cephalosporins (Cef-)
3-Irritant: - I.M. → Painful, so add lidocaine.
4- Nephrotoxicity
Biliary sludge due to insoluble salts in bile
Explain the manifestations of Aminoglycoside (-mycin) toxicity
1.Ototoxicity:
a. Irreversible damage of 8th cranial nerve leading to vertigo & deafness
- Nephrotoxicity:
a. It is usually reversible. - Neuromuscular blockade: It is rare. may result in respiratory muscle paralysis
- Allergic reactions
2 Adverse effects of macrolides (-thromycin or -micin)
Cholestatic Jaundice
Epigastric pain
2 adverse effects of fluoroquinolones (-floxacin)
Photosensitivity
Nephrotoxic
2 adverse effects of Sulfonamides (sulfa-)
Bone marrow inhibition
Stevens-Johnson syndrome in allergy
Two Adverse Effects Rifampicin
Orange-red discoloration of secretions
Allergy → Flu-like syndrome.
Drug interactions of Rifampicin
Hepatic Microsomal Enzyme Inducer→↑ Metabolism of Oral anti-coagulants contraceptives, corticosteroids
2 adverse effects of I.N.H (Isoniazid)
Peripheral neuritis
Hepatotoxicity
Antibacterial Activity of Penicillins
Penicillins: Penicillin G is the prototype (narrow spectrum): All positive cocci, anaerobes, spirochetes, actinomycetes
Extended spectrum Penicillin: Aminopenicillins; gram -ve and Anti-pseudomonal
Therapeutic uses of penicillins
treatments of infections by gram +ve Cocci, gram -ve cocci, gram +ve Bacilli, spirochetes and actinomycosis
Gram -ve bacilli, and pseudomonas
Prophylactic uses: for streptococcal infection in Rheumatic fever, bacterial endocarditis and Gonorrheal neonatal ophthalmia
4 therapeutic uses of cephalosporins
Gram negative meningitis
Gonorrhea
Typhoid fever
UTI
Preparations and Uses Aminoglycosides:
А) Systemic use:
1. Used in serious gram-negative infection and Staphylococcal & Enterococcal infections.
- Bacterial endocarditis. Add Benzyl penicillin.
B) Topical uses:
1. Topical neomycin, in burns, wounds & skin lesions.
2. Oral neomycin for gut decontamination:
C) Uses in TB Streptomycin
4 Therapeutic Uses of Macrolides (-thromycin)
Diphtheria infection
Chlymadia infection
Gonorrheal infection
Syphilitic infection
Therapeutic uses of fluoroquinolones (-floxacin)
- Infections of urogenital caused by gram-negative organisms.
- Respiratory, skin & soft tissue infection.
3 Resistant T.B
5.Typical & atypical pneumonia
Therapeutic Uses of co–trimoxazole (sulfamethoxazole)
1, Respiratory tract infection.
2. Urinary tract infection (UTI).
3. Prostatitis.
4. Salmonella
MOA of Anti-Bacterial Activity of B-lactams : bactericidal
1- They bind to specific Penicillin-Binding-Protein (PBP):
a- y Transpeptidase enzyme responsible for cross-linking of peptidoglycans, a final step in cell wall synthesis → Cell Wall Synthesis.
b-Activate Autolytic enzymes (Autolysins) → Lysis of cell wall.
c- Bacteria imbibe water due to its interior high osmotic pressure → Rupture and DEATH of the microbe.
Explain Antibacterial action of sulphonamide (Sulf-)
Compete with PABA Dihydropteroate synthetase (DHPS) I Folic acid synthesis. Folic acid is essential for synthesis of bacterial purines & DNA.
Anti-Bacterial Activity of Rifampicin
↓ DNA-dependent RNA polymerase enzyme ↓ Synthesis of RNA
Anti-Bacterial Activity of I.N.H. (Isoniazid)
↓ Mycolic acid synthesis —> decrease synthesis of Cell Wall
Mech of action of amphotericin B
Amphotericin B binds to ergosterol in the fungal cell membrane → forming amphotericin B-associated pores in the cell membrane → ↑ permeability of the fungal cell → leakage of fungal cell contents.
Therapeutic uses of amphotericin B
1-Fungal meningitis
2- Fungal pneumonia.
3- Systemic candidiasis
2 adverse effects of amphotericin B
Nephrotoxicity
Seizures after intrathecal administration
Mechanism of action of Azoles (Imidazole)
Inhibit fungal CYP 450 → inhibition of synthesis of ergosterol of fungal cell membrane from lanosterol.
2 Imidazole uses
dandruff
Oral thrush
Mechanism of action Nucleoside reverse transcriptase inhibitor (NRTIs) (-vudine)
mammalian DNA polymerase is relatively resistant.
Mechanism of action Non-Nucleoside reserve transcriptase inhibitors (NNRTIs) (-virine)
Bind to reverse transcriptase near the catalytic site→ denaturation of reverse transcriptase → inhibition of viral DNA production.
MOA of Protease Inhibitors (PIs) (-navir)
Inhibit specific viral protease enzyme essential for cleavage of the synthesized non-functional polyproteins into functional viral proteins.
Mechanism of Action of insulin:
Insulin binds to the a-subunit of tyrosine kinase receptors, → Activation of tyrosine kinase activity of B – subunit → Phosphorylation of intracellular proteins → Change in enzyme activity, gene expression and translocation of Glut-4 transporter→ Glucose uptake by adipose tissue & Skin.
Indications of insulin:
A) Diabetes Mellitus:
1- Type-1 diabetics, all cases of Insulin Dependent Diabetes Mellitus (IDDM)
2- Type2(NIDDM)
3- Emergency treatment of Diabetic Ketoacidosis& Non-ketotic Hyperosmolar Diabetic coma.
B) Other Indications: Hyperkalemia due to renal failure.
Adverse Effects of Insulin:
Hypoglycemia
Hypokalemia
Somogyi Effect > Rebound morning hyperglycemia.
Amylin analog : Pramlintide (Symlin) mechanism of action
i. Reduces glucagon secretion
ii. Delays gastric emptying
iii. Decreases appetite.
Amylin analog Uses:
Used SC in patients with Type 1 or Type 2 diabetes who have problems with postprandial hyperglycemia.
Amylin analog Adverse effects:
anorexia
hypoglycemia
Sulfonylurea (Gly- or Gli-) Mechanism of Action
1- Increase insulin release from the pancreas:
They Block ATP-sensitive K-channel→ Depolarization → Influx of Ca → Exocytosis → ↑Release of Insulin.
2- Other actions (Extra-pancreatic): may increase peripheral insulin sensitivity.
Indications of Sulfonylureas (Gly- or Gli-):
Type-2 Diabetes (NIDD) after failure of Diet regulation &exercise.
a- Non-Obese
b- Non-Complicated Diabetes:
- No stress
- No Major organ disease
Adverse Effects of Sulfonylureas (Gly- or Gli-):
a- Hypoglycemia
b- Weight gain
Mechanism of action of biguanides (-formin; metformin)
1- The primary effect is to reduce hepatic glucose production by activating the enzyme AMP-dependent protein kinase (AMPK). This leads to stimulation of hepatic fatty acid oxidation, glucose uptake, and nonoxidative glucose metabolism and reduction of lipogenesis and gluconeogenesis &glycogenolysis.
Therapeutic Uses of Metformin
● Type 2 , in overweight patients, when dietary management and exercise alone do not result in adequate glycemic control.
● A reduction of diabetic complications after failure of diet
Adverse Effects of Biguanides (-formin; metformin)
↓ absorption of Vitamin B-12.
Rarely fatal Lactic Acidosis may occur so