Drugs Used in Pain and Inflammation Flashcards by Claudia Currie

Corticosteroids

Fludrocortisone

Hydrocortisone

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Fludrocortisone - MOA

Mineralocorticoid.

Acts on electrolyte + H2O metabolism.

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Fludrocortisone - Administration

Oral

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Fludrocortisone - Therapeutic Use

Replaces aldosterone in adrenal insufficiency

Congenital adrenal hyperplasia

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Fludrocortisone - Adverse Effects

Na+ & H2O retention
Hypertension
Oedema
Headache
Hypokalemia
Muscle weakness & fatigue, Immunosuppression
Depression
Weight gain

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Hydrocortisone - MOA

Glucocorticoid.
Anti-inflammatory & immunosuppressant. Metabolic effects [↑ gluconeogenesis, glycogen deposition, & protein / lipid / Ca2+ metabolism]

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Hydrocortisone - Administration

Oral
IV
Topical

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Hydrocortisone - Therapeutic Use

Severe allergic reactions
Eczema
Gout

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Hydrocortisone - Adverse Effects

Dryness

Itching

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Leukotrine Antagonists

Zileuton

Mintelukast

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Zileuton - MOA

Active inhibitor of 5-LOX enzyme. 
Results in inhibition of:
1. LTB4
2.LTC4
3. LTD4
4. LTE4

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Zileuton - Administration

Oral

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Zileuton - Therapeutic Use

Asthma

Allergies (allergic rhinitis)

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Zileuton - Adverse Effects

Sinusitis

Nausea

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Mintelukast - MOA

Leukotriene receptor antagonist

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Mintelukast - Administration

Oral

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Mintelukast - Therapeutic Use

Asthma

Allergies (allergic rhinitis)

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Mintelukast - Adverse Effects

GIT disturbances
Headaches,
Hypersensitivity
Sleep disorders
↑ bleeding

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Non Steroidal Anti-Inflammatories

Aspirin
Diclophenac 
Indomethacin
Piroxicam
Ibuprofen
Naproxen
Mefenamic Acid

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Non Steroidal Anti-Inflammatories - MOA

Competitive, reversible COX I + II inhibition.

Inhibits thromboxane production

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Non Steroidal Anti-Inflammatories - Kinetics

Oral
Rectal
IV
IM

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Non Steroidal Anti-Inflammatories - Therapeutic Use

Analgesic
Anti-inflammatory
Anti-pyretic

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Non Steroidal Anti-Inflammatories - Adverse Effects

Related to PG Inhibition:

GIT effects (ulceration, perforation, bleeding),
Inhibit platelet aggregation resulting in ↑ bleeding time
Renal vasoconstriction leading to ischemia (nephrotoxicity)
Prolonged gestation/bleeding in pregnancy

Unrelated to PG inhibition:

Tinnitus
Hypersensitivity (rash, bronchospasm)

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Non Steroidal Anti-Inflammatories - D/I

Anti-coagulants
Anti-hypertensives
Lithium.

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Aspirin - MOA

Irreversibly acetylates COX I and II

Aspirin - Kinetics

Absorption: Rapid - stomach & small intestine Biotransformation: Liver (glycine conjugation) Excreted: Urine (alkalinity increases)

Aspirin - Therapeutic Use

Analgesic Anti-inflammatory Anti-pyretic In v. low doses: prevent MI/Strokes etc

Aspirin - Adverse Effects

GIT distress | Renal dysfunction

Aspirin - C/I

Children | Pregnancy

Paracetamol - MOA

Reversible, non-competitive inhibition of COX I + II (in brain)

Paracetamol - Kinetics

Rapid absorption | Hepatic conjugation

Paracetamol - Therapeutic Use

Analgesic | Antipyretic

Paracetamol - Adverse Effects

Mild to non-existent. Skin rash Allergic reactions. Acute overdose - hepatic necrosis

Paracetamol - C/I

Hepatic damage

Paracetamol - Administration

Oral IV Rectal

Celecoxib/Etoricoxib - MOA

Cox II selective inhibitor

Celecoxib/Etoricoxib - Administration

Oral

Celecoxib/Etoricoxib - Therapeutic Uses

Osteoarthritis Rheumatoid arthritis Acute pain Menstrual pain

Celecoxib/Etoricoxib - Adverse Effects

``` MI Stroke Renal vasoconstriction Change in BP ↓GFR ```

Celecoxib/Etoricoxib - C/I

Sulfonamide sensitivity

Opioids - Drugs

Codeine | Morphine

Opioids - MOA

Opioid receptor agonist. | Mimics effect of natural endorphins

Opioids - Administration

``` Oral Intrathecal SC IM IV ```

Opioids - Therapeutic Use

Analgesic Antitussive Anti-diarrhoea

Opioids - Adverse Effects

``` Respiratory depression Euphoria Sedation Nausea & vomiting Constipation ```

Histamine Inhibitors

Histamine 1 receptor antagonist (Loratadine) | Xanthines (Theophylline)

Loratadine - MOA

Competitively block receptor-mediated response of target tissue. Does not influence histamine formation or release

Loratadine - Administration

``` Oral Rectal IV IM Topical ```

Loratadine - Therapeutic Use

Allergies | Asthma

Loratadine - Adverse Effects

``` Confusion Drowsiness Dry mouth Respiratory depression Constipation ```

Theophylline - MOA

Phosphodiesterase-4 inhibitor (inflam. cells) | Decreases pulmonary eosinophils

Theophylline - Therapeutic Use

COPD | Asthma

Theophylline - Adverse Effect

``` Nausea Diarrhoea ↑ HR Arrhythmias CNS excitation ```

Theophylline - Administration

Oral | IV

Disease-modifying anti-rheumatoid agents

Methotrexate D-Penicillamine Sulfasalazine

Methotrexate - MOA

Block several immune-related enzymes ∴ affects actively growing cells. Causes immune suppression

Methotrexate - Administration

Oral | IV

Methotrexate - Adverse Effects

Nausea | Vomitting

Methotrexate - Therapeutic Use

↓pain & swelling of arthritis ↓damage to joints ↓long term disability

D-Penicillamine - MOA

``` ↓ T-cells ↓ Macrophage function ↓ IL1 ↓ Rheumatoid factor ↓ Collagen cross-linking ```

D-Penicillamine - Administration

Oral

D-Penicillamine - Therapeutic Use

Immunosuppression | Rheumatoid Arthritis

D-Penicillamine - Adverse Effects

Glomerulonephritis | Myasthenic syndrome

Sulfasalazine - MOA

↓ Synthesis of inflammatory mediators

Sulfasalazine - Administration

Oral

Sulfasalazine - Therapeutic Use

Rheumatoid arthritis Inflammatory bowel disease Ulcerative colitis

Sulfasalazine - Adverse Effects

Depression | Infertility

Gout Treatment

Colchichine Allopurinol Probenecid

Colchichine - MOA

Mitotic poison

Colchichine - Administration

Oral

Colchichine - Therapeutic Use

Gout

Colchichine - Adverse Effects

GIT effects | Neutropenia

Allopurinol - MOA

Inhibits xanthine oxidase

Allopurinol - Administration

Oral

Allopurinol - Therapeutic Use

Gout (over-secretors)

Allopurinol - Adverse Effects

Skin Rash Eosinophillia Hepatitis

Probenecid - MOA

Interferes with kidney’s organic anion transporter

Probenecid - Administration

Oral

Probenecid - Adverse Effects

Increases serum levels of some antimicrobials

Probenecid - Therapeutic use

Gout (under-secretors)

Anesthetics

Nitrous Oxide | Lignocaine/Procaine

Nitrous Oxide - MOA

Neuromuscular blocker

Nitrous Oxide - Administration

Inhaled

Nitrous Oxide - Therapeutic Use

Pain suppressant | General anesthetic

Nitrous Oxide - Adverse Effects

Neurotoxicity

Lignocaine/Procaine - MOA

Reversibly block impulse cond. along axons | Prevents Na+ conduction (no APs)

Lignocaine/Procaine - Administration

IV SC Topical

Lignocaine/Procaine - Therapeutic Use

Local anesthetic

Lignocaine/Procaine - Adverse Effects

Rare (excessive exposure causes CNS & CVS effects)