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Drug Class

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30 views12 pages

Drug Class

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Fallen Angel
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
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Drug Class: NSAID

Drug Name: Diclofenac Sodium


Pharmaceutical Form: Tablet – (Enteric coated 50mg, Dispersible 50mg, Sustained
release100mg,)/Injection (75mg)/Topical Gel (1% or 3%).

Brands: Dicloran, Artifen, Voltral.


Mechanism Of Action:
 Inhibits cyclooxygenase (COX) enzymes.
 Reduces prostaglandin synthesis.
Indications:
 Arthritis.
 Relief of pain and inflammation due to trauma.
 Acute musculoskeletal disorders.
Dosage:
 Adults:75mg to 150mg a day, given in two or three divided doses.
 Maximum dose: 150mg a day.
 Children: 1mg/kg to 3mg/kg a day, given in divided doses.
Bioavailability: Oral:
 Approximately 50-60%
 Subject to first-pass metabolism

Intravenous (IV):
 100% (by definition for IV route).
Adverse Drug Reaction:
 Gastrointestinal: Ulcers, bleeding, perforation
 Cardiovascular: Increased risk of heart attack and stroke
 Renal: Impaired kidney function
Interactions:
 Other NSAIDs: Increased risk of GI side effects
 Anticoagulants (e.g., warfarin): Increased bleeding risk
 Antiplatelets (e.g., aspirin): Increased bleeding risk

Contraindications:
 Children under 6 months
Cerebrovascular disorder
Gastrointestinal haemorrhage
Gastrointestinal perforation
Gastrointestinal ulcer
History of gastrointestinal haemorrhage
History of peptic ulcer

Pregnancy and Lactation: Pregnancy category: C (first and second trimesters), D (third
trimester). Lactation:
 Excreted in breast milk in small amounts
 Generally considered compatible with breastfeeding.
Toxicity:
 Gastrointestinal symptoms: Nausea, vomiting, abdominal pain
 CNS effects: Headache, dizziness, drowsiness
 Cardiovascular: Hypertension, tachycardia
 Renal: Acute kidney injury
 Metabolic: Metabolic acidosis
Management: While there is no specific antidote for diclofenac toxicity, management
focuses on supportive care and symptom treatment:
1. Discontinue diclofenac immediately
2. Gastric decontamination (if recent ingestion):
o Activated charcoal
o Gastric lavage (in severe cases)
3. Supportive care:
o IV fluids for hydration and to support renal function
o Oxygen therapy if needed
o Monitor vital signs
IV Stability: Before reconstitution:
1. Unopened vials: Stable at room temperature (20-25°C)
2. Protect from light
3. Do not freeze
4. Shelf life typically 2-3 years (check manufacturer's specifics)
After reconstitution:
1. Chemical stability: 24 hours at room temperature (20-25°C)
2. Microbiological stability: Use immediately after preparation
3. If not used immediately, in-use storage times should not exceed 24 hours at 2-8°C
(refrigerated)
4. Protect from light
Diluents Compatibility:
 Compatible with 0.9% sodium chloride or 5% glucose solutions
 Do not mix with other medications in the same infusion
Dose Adjustment in Renal and Hepatic Insufficiency: Hepatic impairment:
1. Mild to moderate: No initial dose adjustment needed, but monitor closely
2. Severe: Avoid use if possible; if necessary, use lowest effective dose
3. Monitor liver function regularly
Renal impairment:
1. Mild (GFR 60-89 mL/min): No dose adjustment needed
2. Moderate (GFR 30-59 mL/min): Use with caution, start with lower doses
3. Severe (GFR <30 mL/min): Avoid use if possible; if necessary, use lowest effective
dose
4. Monitor renal function regularly.

References
www.medscape.co.uk.com
www.medicines.org.uk.com
www.drugs.com

Drug Class: Antihypertensive


Drug Name: Bisoprolol fumarate
Pharmaceutical form: Tablet 2.5mg,5mg,10mg
Brands: Barilol, Concor, Actim
Mechanism of Action: Selective β1-adrenergic receptor antagonist:
 Primarily blocks β1 receptors in the heart

Indications:  Hypertension (high blood pressure)


 As monotherapy or in combination with other antihypertensives
 Chronic heart failure
 To reduce mortality and hospitalizations in stable patients
 Coronary artery disease
 For secondary prevention after myocardial infarction
 Management of stable angina pectoris
Dosage:
 Adults: The usual recommended dose is 10 mg once daily
 Maximum dose: Maximum recommended dose is 20 mg once daily
 Children: Not recommended

Bioavailability: Oral bioavailability: Approximately 90%


 High bioavailability due to low first-pass metabolism
Adverse Drug Reactions: Cardiovascular:
 Bradycardia
 Hypotension
 AV block
 Worsening of heart failure (initially)
Respiratory:
 Bronchospasm (rare due to β1 selectivity, but possible in susceptible patients)
Interactions:  Other beta-blockers:
 Enhanced beta-blocking effects
 Calcium channel blockers (esp. verapamil, diltiazem):
 Increased risk of bradycardia, AV block, hypotension
 Antiarrhythmics (e.g., amiodarone, disopyramide):
 Increased risk of bradycardia, conduction disturbances
 Digoxin:
 Increased risk of bradycardia
Contraindications:
Children under 18 years
Acute cardiac failure
Bradycardia with pulse rate at rest < 60bpm before treatment
Breastfeeding
Cardiogenic shock
Pregnancy And Lactation: Pregnancy:
1. FDA Pregnancy Category: C
Lactation:
1. Can be excreted in small amounts in breastmilk. Use not recommended.
Toxicity: Acute toxicity:
1. Cardiovascular effects:
o Severe bradycardia
o Hypotension
o AV block
o Cardiogenic shock
o Cardiac arrest (in severe cases)
2. Central Nervous System:
o Dizziness
o Confusion
o Seizures (rare)
o Coma (in severe overdose)
3. Respiratory:
o Bronchospasm (especially in patients with underlying respiratory disease)
o Respiratory depression
4. Metabolic:
o Hypoglycaemia
o Hypokalaemia
5. Other:
o Nausea, vomiting
o Cold extremities
Management:
 Supportive care and monitoring
 Activated charcoal if recent ingestion
 Atropine for bradycardia
 IV fluids for hypotension
 Glucagon for refractory bradycardia and hypotension
 Consider cardiac pacing in severe cases
 Beta-agonists (e.g., isoproterenol) for severe bradycardia unresponsive to other
measures
 Haemodialysis is generally not effective due to high protein binding

References
www.medscape.co.uk.com
www.medicines.org.uk.com
www.drugs.com
Drug Class: Antibiotic
Drug Name: Co-Amoxiclav
Pharmaceutical form:
Tablet (375mg,625mg,1000mg)/Suspension(156.25mg/5ml,312.5ml/5ml)/Parenteral
Brands: Calamox, Augmentin, Amoxi-Clav
Mechanism of Action:
1.Amoxicillin:
 A beta-lactam antibiotic from the penicillin family
 Inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs)
 This disrupts peptidoglycan cross-linking, leading to cell lysis and death
2. Clavulanic acid:
 A beta-lactamase inhibitor
 Binds irreversibly to beta-lactamase enzymes produced by some bacteria
 Prevents these enzymes from inactivating amoxicillin
Indications: 1. Respiratory tract infections:
 Acute sinusitis
 Acute otitis media
 Acute exacerbations of chronic bronchitis
 Community-acquired pneumonia
2. Skin and soft tissue infections:
 Cellulitis
 Animal bites
 Severe dental abscesses with spreading cellulitis
3. Urinary tract infections:
 Complicated UTIs
 Pyelonephritis
4. Gynaecological infections:
 Pelvic inflammatory disease
5. Intra-abdominal infections:
 Peritonitis
 Diverticulitis
6. Bone and joint infections:
 Osteomyelitis
7. Prophylaxis:
 Surgical prophylaxis in some procedures, particularly those involving the
gastrointestinal tract
Dosage: Adults: 2g co-amoxiclav (1g amoxicillin/200mg clavulanic acid) every 8 hours or
2.2g co-amoxiclav (2g amoxicillin/200mg clavulanic acid) every 12 hours.
Maximum dose: 2.2g co-amoxiclav every 8 hours
Children:  For mild to moderate infections: • 20-40 mg/kg/day divided into 3 doses
 For severe infections: • 40-90 mg/kg/day divided into 2-3 doses
Bioavailability:  Oral bioavailability: Approximately 90%
 Absorption is not significantly affected by food

Adverse Drug Reactions:


 Gastrointestinal:
 Diarrhea
 Nausea
 Vomiting
 Indigestion
 Skin:
 Rash
 Pruritus (itching)
Interactions:
 Anticoagulants:
 Warfarin and other oral anticoagulants: May increase INR, requiring close monitoring
 Contraceptives:
 May reduce effectiveness of oral contraceptives
 Methotrexate:
 Increased risk of methotrexate toxicity due to reduced renal clearance
 Probenecid:
 Increases and prolongs serum levels of amoxicillin (but not clavulanic acid)
Contraindications:
 Infectious mononucleosis
History of drug induced hepatic impairment
History of drug induced jaundice

Pregnancy and Lactation: FDA Pregnancy Category: B


 Animal studies show no risk, but adequate human studies are lacking
Lactation:
1. Safety:
o Generally considered safe during breastfeeding
2. Excretion in breast milk:
o Both amoxicillin and clavulanic acid are excreted in small amounts
Toxicity: Chronic Toxicity:
1. Liver toxicity:
o Most significant concern with prolonged use
o Cholestatic hepatitis (more common than with amoxicillin alone)
o Risk factors: elderly, prolonged treatment (>14 days), male gender
2. Renal toxicity:
o Rare but can occur, especially with high doses or in patients with pre-existing
renal impairment
o Manifestations: interstitial nephritis, crystalluria
Management:
 Supportive care
 Gastric decontamination if recent ingestion
 Monitor renal function and electrolytes
 Haemodialysis can be considered in severe cases

IV Stability:  Reconstitution:
 Should be reconstituted immediately before use
 Use sterile water for injection or compatible diluents as specified in the product
information
 Stability after reconstitution:
 Generally stable for 20-30 minutes at room temperature (20-25°C)
 Stability can vary depending on the specific formulation and concentration
 Infusion stability:
 In most common IV fluids (e.g., normal saline, lactated Ringer's): • Stable for 2-3
hours at room temperature • Stable for up to 8 hours if refrigerated (2-8°C)
Diluents Compatibility:
 0.9% Sodium Chloride (Normal Saline)
 Lactated Ringer's Solution
 5% Dextrose in Water (at lower concentrations of co-amoxiclav)
 0.45% Sodium Chloride

Dose Adjustments:
 Mild renal impairment (CrCl 30-60 mL/min):
 No dosage adjustment usually required
 Monitor renal function closely
 Moderate renal impairment (CrCl 10-30 mL/min):
 Oral: 500 mg/125 mg every 12 hours
 IV: 1000 mg/200 mg every 12 hours
 Severe renal impairment (CrCl <10 mL/min):
 Oral: 500 mg/125 mg every 24 hours
 IV: 1000 mg/200 mg every 24 hours

References
 www.medscape.co.uk.com
 www.medicines.org.uk.com
 www.drugs.com
Drug Class: Anti-Diabetic
Drug Name: Metformin
Pharmaceutical form: Tablet (250mg,500mg,850mg,1g)
Brands: Glucophage, Neodipar, Metphage

Mechanism of Action: Increased insulin sensitivity:

 Enhances peripheral glucose uptake, particularly in skeletal muscle


 Improves insulin receptor binding and post-receptor signalling
Indications:
 Type 2 Diabetes Mellitus:
 First-line pharmacological therapy for most patients
 Used as monotherapy or in combination with other antidiabetic agents
 Prediabetes:
 To prevent progression to type 2 diabetes in high-risk individuals
 Polycystic Ovary Syndrome (PCOS):
 To improve insulin sensitivity and reduce androgen levels
 May help regulate menstrual cycles and improve fertility
 Gestational Diabetes:
 Sometimes used as an alternative to insulin during pregnancy

Dosage: Adults: Initial dosing:


 Usually start with 500 mg twice daily with meals
 Alternatively, can start with 850 mg once daily
Maximum: 2550 mg daily
Children: immediate-Release (IR) Tablets:

 Initial dose: 500 mg twice daily


 Maximum dose: 2000 mg daily in divided doses
Bioavailability:  Metformin’s absolute bioavailability ranges between 40% to 60%. This
means that when a dose is taken orally, only 40-60% of the active drug enters the
bloodstream to exert its therapeutic effects.
Adverse Drug Reaction: Gastrointestinal (GI) Disturbances:
 Nausea: A frequently reported side effect, particularly when starting the medication.
 Diarrhea: This can be persistent and often leads to dose adjustment or
discontinuation.
 Abdominal Pain: Some patients experience stomach cramps or discomfort.
 Bloating and Flatulence: These symptoms are part of the GI intolerance experienced
by some individuals.
Interactions: Drug-Drug Interactions
a. Drugs Affecting Absorption
 Cationic Drugs:
o Examples: Cimetidine, Ranitidine, Trimethoprim.
o Effect: Compete with metformin for absorption in the gut, potentially
reducing its effectiveness.
o Management: Monitor blood glucose levels; adjust metformin dose if needed.
 GI Motility Modifiers:
o Examples: Anticholinergics (atropine), Opioids (morphine).
o Effect: Alter gastrointestinal motility, impacting metformin absorption.
o Management: Monitor blood glucose and GI symptoms.
b. Drugs Affecting Renal Clearance
 Diuretics: (e.g., Furosemide)
o Effect: Can impair renal function, increasing metformin levels and risk of
lactic acidosis.
o Management: Monitor renal function; adjust metformin dose as needed.
 NSAIDs: (e.g., Ibuprofen)
o Effect: May reduce renal function, affecting metformin clearance.
o Management: Monitor renal function; adjust dose accordingly.
 ACE Inhibitors: (e.g., Enalapril)
o Effect: Can impair renal function.
o Management: Regular renal function monitoring.
c. Drugs Affecting Metabolic Control
 Corticosteroids: (e.g., Prednisone)
o Effect: Increase blood glucose, opposing metformin’s effect.
o Management: Monitor blood glucose; adjust metformin dose during
corticosteroid therapy.
 Thyroid Hormones: (e.g., Levothyroxine)
o Effect: Increase blood glucose, reducing metformin’s effectiveness.
o Management: Monitor blood glucose; adjust dose if needed.
 Insulin and Insulin Secretagogues: (e.g., Glipizide, Glyburide)
o Effect: Increase risk of hypoglycemia.
o Management: Careful monitoring of blood glucose; adjust doses of
concomitant medications.
d. Drugs Increasing Lactic Acidosis Risk
 Alcohol:
o Effect: Increases risk of lactic acidosis, particularly with acute or chronic use.
o Management: Advise patients to limit alcohol intake.

Contraindications: Renal Impairment


Severe Renal Dysfunction:
 Definition: Metformin is contraindicated in patients with severe renal impairment
because it is primarily excreted unchanged by the kidneys.
. Liver Disease
Hepatic Impairment:
 Definition: Metformin is contraindicated in patients with significant hepatic dysfunction.
 Rationale: The liver is crucial for lactate clearance; impairment can increase the risk of lactic
acidosis.
 Conditions:
o Cirrhosis
o Acute liver failure
o Severe hepatic steatosis (fatty liver)

Metabolic Acidosis
Diabetic Ketoacidosis (DKA) and Lactic Acidosis:
 Definition: Metformin is contraindicated in patients with metabolic acidosis, including DKA
and lactic acidosis.
 Rationale: Metformin can worsen metabolic acidosis and is itself a risk factor for lactic
acidosis.
Pregnancy and Lactation: Generally safe to use.
Dose Adjustments: Hepatic impairment: Avoid use; risk of lactic acidosis
Renal impairment:
 Obtain eGFR before starting metformin
 eGFR <30 mL/min/1.73 m²: Contraindicated
 eGFR 30-45 mL/min/1.73 m²: Not recommended to initiate treatment
 Monitor eGFR at least annually or more often for those at risk for renal impairment (eg,
elderly)
 If eGFR falls below 45mL/min/1.73 m² while taking metformin, risks and benefits of
continuing therapy should be evaluated
 If eGFR falls below 30 mL/min/1.73 m² while taking metformin, discontinue drug

Drug Class: Multi-Vitamin


Drug Name: Calcium + Vitamins D3+C+B6
Pharmaceutical form: Effervescent tablet
Brand: Cac- 1000 Plus
Mechanism of Action:  Antioxidant activity:
 Vitamin C act as antioxidants, protecting cells from oxidative stress.
 Metabolic support:
 B-vitamins play crucial roles in energy metabolism and cellular function.
 Cellular growth and repair:
 Vitamins C and D support cell growth, differentiation, and repair processes.
Indications:
 Calcium deficiency
 Vitamin deficiencies
 Hypocalcemia
 Osteomalacia
 Osteoporosis
 Pregnancy and lactation
 Rickets
Dosage: Adult & Children (above 7) ......... 1 Tablet daily.
Children 3-7 years ..................... ½ Tablet daily.

Side effects: The common side effects of CaC-1000 Plus are:


 Nausea
 Diarrhea
 Hypercalcemia
 Constipation
Contraindications: Kidney stones:
People with a history of kidney stones, or with a family history of kidney stones should take CaC
1000 upon consultation with their doctor. While CaC 1000 is safe for patients with kidney stones or a
history thereof, it can still increase the propensity towards the development of kidney stones and
should be used with caution.

 Hypercalcemia:

Hypercalcemia refers to raised levels of calcium in the blood. There are various reasons behind this
spike, including dehydration, thyroid disease, and malignancy. Severe hypercalcemia can result in
osteoporosis, kidney stones, kidney failure, impaired nervous system, and arrhythmia. Thus, people
with hypercalcemia should take CaC 1000 with caution

 Heart patients:
People with a history of heart diseases like angina and heart attack should consult their doctor before
taking CaC 1000. As calcium supplements can increase the risk of heart diseases, therefore, people
should confer with an expert first.

 Stroke:
According to research, calcium supplements can increase the risk of stroke. Individuals with a family
history of stroke are therefore suggested to consult their healthcare provider before using CaC 1000.

 Altered kidney function:


Our kidneys process waste products and toxins. When they are not working at full capacity, due to
any disease or disorder, this processing ability gets compromised

Interactions: CaC-1000 Plus can interact with the following drugs:

 Ceftriaxone
 Quinolone antibiotics
 Tetracycline antibiotics
 Bisphosphonates
 Calcipotriene
 Digoxin
 Diltiazem
 Levothyroxine
 Sotalol
 Thiazide diuretics- hydrochlorothiazide
 Calcium channel blockers like verapamil
 Lithium
 Estrogens
Pregnancy and Lactation: Although it is safe to take CaC-1000 Plus during pregnancy and
lactation, caution must be observed when administering higher doses. Follow the instructions given
by your healthcare provider.

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