Written Pharmacology Flashcards

1
Q

2 Adverse Effects of Penicllins:

A

Allergic Reactions: angioedema & Anaphylactic shock

CNS irritation (seizures) may occur with large doses in patients with renal failure

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2
Q

Discuss Toxicity of Cephalosporins (Cef-)

A

3-Irritant: - I.M. → Painful, so add lidocaine.

4- Nephrotoxicity

Biliary sludge due to insoluble salts in bile

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3
Q

Explain the manifestations of Aminoglycoside (-mycin) toxicity

A

1.Ototoxicity:
a. Irreversible damage of 8th cranial nerve leading to vertigo & deafness

  1. Nephrotoxicity:
    a. It is usually reversible.
  2. Neuromuscular blockade: It is rare. may result in respiratory muscle paralysis
  3. Allergic reactions
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4
Q

2 Adverse effects of macrolides (-thromycin or -micin)

A

Cholestatic Jaundice
Epigastric pain

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5
Q

2 adverse effects of fluoroquinolones (-floxacin)

A

Photosensitivity
Nephrotoxic

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6
Q

2 adverse effects of Sulfonamides (sulfa-)

A

Bone marrow inhibition
Stevens-Johnson syndrome in allergy

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7
Q

Two Adverse Effects Rifampicin

A

Orange-red discoloration of secretions
Allergy → Flu-like syndrome.

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8
Q

Drug interactions of Rifampicin

A

Hepatic Microsomal Enzyme Inducer→↑ Metabolism of Oral anti-coagulants contraceptives, corticosteroids

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9
Q

2 adverse effects of I.N.H (Isoniazid)

A

Peripheral neuritis
Hepatotoxicity

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10
Q

Antibacterial Activity of Penicillins

A

Penicillins: Penicillin G is the prototype (narrow spectrum): All positive cocci, anaerobes, spirochetes, actinomycetes

Extended spectrum Penicillin: Aminopenicillins; gram -ve and Anti-pseudomonal

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11
Q

Therapeutic uses of penicillins

A

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

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12
Q

4 therapeutic uses of cephalosporins

A

Gram negative meningitis
Gonorrhea
Typhoid fever
UTI

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13
Q

Preparations and Uses Aminoglycosides:

A

А) Systemic use:
1. Used in serious gram-negative infection and Staphylococcal & Enterococcal infections.

  1. 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

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14
Q

4 Therapeutic Uses of Macrolides (-thromycin)

A

Diphtheria infection
Chlymadia infection
Gonorrheal infection
Syphilitic infection

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15
Q

Therapeutic uses of fluoroquinolones (-floxacin)

A
  1. Infections of urogenital caused by gram-negative organisms.
  2. Respiratory, skin & soft tissue infection.

3 Resistant T.B

5.Typical & atypical pneumonia

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16
Q

Therapeutic Uses of co–trimoxazole (sulfamethoxazole)

A

1, Respiratory tract infection.
2. Urinary tract infection (UTI).
3. Prostatitis.
4. Salmonella

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17
Q

MOA of Anti-Bacterial Activity of B-lactams : bactericidal

A

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.

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18
Q

Explain Antibacterial action of sulphonamide (Sulf-)

A

Compete with PABA Dihydropteroate synthetase (DHPS) I Folic acid synthesis. Folic acid is essential for synthesis of bacterial purines & DNA.

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19
Q

Anti-Bacterial Activity of Rifampicin

A

↓ DNA-dependent RNA polymerase enzyme ↓ Synthesis of RNA

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20
Q

Anti-Bacterial Activity of I.N.H. (Isoniazid)

A

↓ Mycolic acid synthesis —> decrease synthesis of Cell Wall

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21
Q

Mech of action of amphotericin B

A

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.

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22
Q

Therapeutic uses of amphotericin B

A

1-Fungal meningitis
2- Fungal pneumonia.
3- Systemic candidiasis

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23
Q

2 adverse effects of amphotericin B

A

Nephrotoxicity
Seizures after intrathecal administration

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24
Q

Mechanism of action of Azoles (Imidazole)

A

Inhibit fungal CYP 450 → inhibition of synthesis of ergosterol of fungal cell membrane from lanosterol.

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25
2 Imidazole uses
dandruff Oral thrush
26
Mechanism of action Nucleoside reverse transcriptase inhibitor (NRTIs) (-vudine)
they form abnormal DNA chains leading to termination of viral DNA production
27
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.
28
MOA of Protease Inhibitors (PIs) (-navir)
Inhibit specific viral protease enzyme essential for cleavage of the synthesized non-functional polyproteins into functional viral proteins.
29
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.
30
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.
31
Adverse Effects of Insulin:
Hypoglycemia Hypokalemia Somogyi Effect > Rebound morning hyperglycemia.
32
Amylin analog : Pramlintide (Symlin) mechanism of action
i. Reduces glucagon secretion ii. Delays gastric emptying iii. Decreases appetite.
33
Amylin analog Uses:
Used SC in patients with Type 1 or Type 2 diabetes who have problems with postprandial hyperglycemia.
34
Amylin analog Adverse effects:
anorexia hypoglycemia
35
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.
36
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
37
Adverse Effects of Sulfonylureas (Gly- or Gli-):
a- Hypoglycemia b- Weight gain
38
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.
39
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
40
Adverse Effects of Biguanides (-formin; metformin)
↓ absorption of Vitamin B-12. Rarely fatal Lactic Acidosis may occur so
41
Mechanism of action of GLP-1 analogues (-glutide)
1- Synthetic analogs of Glucagon-like Peptide-1 → Bind to GLP-1 receptors → reduce postprandial glucose elevation and glucagon levels, delay gastric emptying, ↑ insulin release & and suppress appetite
42
Uses GLP-1 analogue (-glutide)
1- control glycemia in patients with type 2 diabetes who fail to achieve control via metformin and/or sulfonylureas. 2- Liraglutide for weight loss.
43
Disadvantages GLP-1 analogues (-glutide)
Pancreatitis renal impairment and acute renal injury may occur
44
DPP-4 (-gliptin) mechanism of action
release of (DPP-4) enzyme leading to prolongation of the action of endogenously released glucose independent peptide
45
Adverse Effects of DDP-4 (-gliptin)
1- Infrequent pancreatitis 2- increase risk of heart failure
46
SGLT2 INHIBITORS (-gliflozin) Mechanism of action
inhibiting this transporter will result in glucose excretion of only 30- 50% of the amount filtered causing glycosuria and lowers glucose levels in patients with type 2 diabetes.
47
Clinical indication of SGLT-2 inhibitors (-gliflozin)
Used as 3rd line therapy for type 2 DM
48
SGLT-2 inhibitors (-gliflozin) Adverse effects:
1. Genital & urinary tract infections 2. Hypotension
49
Mechanism of action of thyroid hormones:
1. T3 and T4 dissociate from Thyroxine-binding globulin (TBG) and enter cells by diffusion or active transport. 2. Inside the cell, T4 deiodinated to T3 3. T3 enters the nucleus and attaches to its nuclear receptor 4. Drug-receptor complex bind to DNA and promotes transcription of specific gens mRNA formation → synthesis (production of various enzymes).
50
Therapeutic Uses of Thyroid Hormones:
1. Replacement therapy in hypothyroidism 2. TSH suppression therapy in thyroid cancer and nontoxic goiter.
51
Mechanism of Action Thioamides (Propylthiouracil)
1. Inhibition of oxidation of iodide to iodine. 2. Inhibition of iodide organification 3. Inhibition of coupling of iodotyrosines to T4 and T3. 4. Propylthiouracil in addition reduces conversion of T4 to T3 in the periphery.
52
Therapeutic uses Thioamides (Propylthiouracil)
1. As principal therapy. 2. As adjuvant to I 131 to control the disease while waiting its effect. 3. To control the disorder in preparation for surgical treatment. 4. Thyroid storm
53
Adverse effects of Thioamides (Propylthiouracil)
Hepatotoxicity Agranulocytosis
54
Iodides Mechanism of action :
1. Inhibition of iodide organification 2. Reduction of the response of thyroid gland to TSH, 3. Inhibition Release of T3& T4.
55
Iodides Therapeutic indications :
Preparation of the patient for thyroidectomy Prophylactic where goiter is endemic.
56
Iodides Adverse effects
1. iodism: metallic taste, painful salivary glands, excess salivation, running eyes &nose. 2. Allergic reactions: angioedema, rash, drug fever
57
Therapeutic uses of estrogens
1. Contraception with progestogens. 2. Postmenopausal hormonal therapy(HT): 3. Replacement therapy: a. 1ry hypogonadism (ovarian failure). b. Premature menopause c. Surgical menopause
58
Adverse Effects of estrogens
Thromboembolic events myocardial infarction.
59
Therapeutic uses of progestins
1. Oral contraception: alone or with estrogen 2. Functional uterine bleeding. 3. Dysmenorrhea, Amenorrhea, Endometriosis.
60
Adverse Effects of progestins
Edema Psychic depression.
61
Uses of androgens
Replacement therapy in male 1ry hypogonadism
62
Adverse effects of androgens:
masculinization in females, hirsutism early puberty and premature closure of epiphyseal plates in children.
63
Mechanism of action of cortisol
Binds to cytoplasmic glucocorticoids receptor---> activation---> receptor hormone complex ---> acts as a transcription factor to express or repress genes
64
Uses of Glucocorticoids
A) Replacement therapy in adrenocortical insufficiency (Addison'sdisease) : a) Acute Addisonian Crisis: b) Chronic Addison's Disease: B) Supplementary & Suppressive therapy 1. Anti-Inflammatory 2. Allergic diseases 3. Immunosuppressive in: Auto-immune diseases 4. shock and stress conditions
65
Adverse Effects of Glucocorticoids:
Moon face & Buffalo hump Cataract & increases intra-ocular pressure ›-Glaucoma. Na retention: Edema and Hypertension
66
Contraindications of Glucocorticoids
Hypertension Peptic ulcer. Glaucoma
67
Calcitonin Action:
* Hypocalcemic hormone * Decreases Ca++ level in the blood 1) Bone: inhibits osteoclastic activity so, it decreases bone resorption. 2) Kidney: inhibits calcium and phosphate reabsorption by the kidney tubules
68
Calcitonin 2 uses
- relief of pain associated with osteoporotic fracture. - may be beneficial in patients who have recently suffered a vertebral fracture.
69
Action of biphosphonates
decrease osteoclastic bone resorption
70
Adverse effects of biphosphonates:
Esophagitis and esophageal ulcers.
71
Adverse Effects of Vancomycin
Nephrotoxic. Rapid VI infusion →Histamine release → Red man syndrome & Shock.
72
Adverse Effects of Tetracyclines (-cycline)
2. Teeth & Bone Abnormalities - avoided during pregnancy, and lactation & in children up to 18 years. 3. Hepatotoxicity during pregnancy
73
Adverse Effects of Co-trimoxazole
Allergy Nephrotoxicity
74
Therapeutic Uses of Vancomycin
1. IV in MRSA & Enterococcal infections. 2. IV prophylactic before dental operations in patients with prosthetic valves. 3. Orally in pseudomembranous colitis.
75
Therapeutic Uses of Tetracyclines (-cycline)
Sinusitis Amoebic dysentery Acne Cholera
76
Therapeutic Uses of Rifampicin
1. First line drug in T.B. 2. Leprosy. 3. Drug of choice in prophylaxis of Meningococcal meningitis
77
Mechanism of Action of Vancomycin
Inhibits early steps of Cell wall synthesis →Peptidoglycan polymerization →Bactericidal.
78
Mechanism of Action of Aminoglycoside :
1. They bind to 30 S ribosomal subunit leading to inhibition of bacterial protein synthesis
79
4 uses of benzodiazepines (-azepam)
Anti epileptic Anti convulsant Anti anxiety Anti depressant Anesthesia
80
2 adverse effects of benzodiazepines (-azepam)
Sedation Addiction
81
SSRI (-oxetine) 4 uses and two adverse effects
Eating disorder (AE anorexia) Depression (Serotonin syndrome) PTSD Panic
82
MOA of L-Dopa
L-DOPA by Central Dopa Decarboxylase →Dopamine > increase D2 receptors
83
L-Dopa uses
treats all manifestation of Parkinsonism by tremors by stimulating D2 receptors in basal ganglia
84
L-Dopa side effects
Sudden with drawl causes Severe rigidity Delusions and hallucinations
85
Anti-epileptics MOA
Increase inhibitory trans (GABA) decrease excitatory (glutamate)
86
Phenytoin uses
Grand mal partial seizures Status Epilepticus
87
MOA and USES of Carbamazepine (-azepine)
Blocks Na channels, thereby inhibiting repetitive action potentials in epileptic focus Uses: Grand Mal Epilepsy & Partial seizures Trigeminal neuralgia Mood stabilizer
88
Adverse effects of Carbamazepine (-azepine)
Steven-johnson syndrome Bone marrow inhibition
89
Phenytoin adverse effects
Convulsions Vertigo
90
Morphine MOA and USES
Morphine stimulates specific Opioid= Opiate receptors in CNS & Periphery Uses: Cancer pain, Colic pain ,Cardiac Pain, Post operative pain
91
Morphine adverse effects
Pin point pupil (PPP) Inhibition of Respiration Interfere with proper diagnosis of Head injury
92
Aspirin (Salicylates) actions and uses
Anti-inflammatory-----> superficial pains Anti- Rheumatic-----> for arthritis Anti-platelet-----> thromboembolic disease Increase uric acid secretion-----> chronic gout
93
MOA of Aspirin (Salicylates):
irreversible inhibition of COX enzyme (1,2,3) by acetylation.
94
MOA of paracetamol and uses
1. Inhibit COX-3 in C.N.S. Mainly Anti-pyretic Analgesic →As potent as Aspirin. Allergy to aspirin, bronchial asthma, peptic ulcer
95
Adverse Effects of Paracetamol
Nephrotoxicity Allergy
96
Therapeutic Uses of Colchicine
1. Useful when NSAIDs & corticosteroids are contraindicated or not tolerated. 2. Prophylaxis of Gout 3. Prophylaxis of Familial Mediterranean Fever
97
MOA of Allopurinol
1. Allopurinol is metabolized by Xanthine Oxidase enzyme (XOE) → Aloxanthine. 2. Both Alopurinol & Aloxanthine →Occupy & inhibits X.E. →deceases Synthesis of uric acid.
98
Uses of Allopurinol
Gouty nephropathy urate renal stones.
99
Adverse Effects of Allopurinol
Allergic skin reaction (mainly rash) Hepatomegaly.
100
Adverse effects and toxicity of LA:
A- Systemic toxicity: 1. CNS a. restlessness, tremors. b. This is followed by respiratory depression, coma, and death from respiratory failure. 2. Cardiovascular system a. Bradycardia. b. Hypotension B- Local toxicity 1. Nerve damage →prolonged sensory &motor loss. 2. Tissue damage →necrosis due to VC by adrenaline added to LA. C- Toxicity of spinal anaesthesia: a. Hypotension b. Treatment by leg elevation - I.V. fluid - sympathomimetics.
101
Teriparatide MOA and uses
* It is administered once-daily by subcutaneous injection with a net effect of stimulating new bone formation leading to increased bone mineral density * Uses: Treatment of osteoporosis.