IPS2: Pharmacology - Part 6.3.1 - Drugs for Rheumatologic Disorder - Introduction, Non-Narcotic Analgesics

Rheumatologic disorder can be

a. Inflammatory

b. Autoimmune disease

c. Both

d. None

c. Both

True about inflammation except:

a. A non-specific immune response against an adverse stimulus

b. Can be caused by microbial invasion

c. Can be caused by physical Injury

d. Main purpose is for body's protection and a part of healing process

e. None

e. None

Cardinal signs of inflammation except:

a. Calor: Heat

b. Rubor: Redness

c. Tumor: Swelling

d. Dolor: Pain

e. Functio laesa: Loss of Function

f. None

f. None

Autoimmune diseases except:

a. Conditions that arise from overreactive immune responses

b. Involved T cells and B cells

c. T cells and B cells → tend to be self-reactive meaning they can adversely target substances & tissues normally present in the body

d. T cells and B cells are designed to address foreign threats but instead they target our own cells leading to abnormality called autoimmune diseases

e. None

e. None

Rheumatologic disorders affect muscoskeletal system including the following except:

a. Joints

b. Muscles

c. Bones

d. Tendons

e. Ligaments

f. None

f. None

Rheumatologic disorder:

Characterized by chronic and systemic inflammation affecting synovium.

a. Rheumatoid Arthritis (RA)

b. Osteoarthritis

c. Systemic Lupus Erythematosus

d. Ankylosing Spondylitis

a. Rheumatoid Arthritis (RA)

Rheumatoid Arthritis (RA)

a. Multiple and symmetrical affecting

b. Morning joint stiffness that last for ~1hr

c. There is hand involvement

d. a and b

e. b and c

f. All

f. All

Rheumatologic disorder:

Most common joint disease in humans that is not inflammatory, and not autoimmune disease.

a. Rheumatoid Arthritis (RA)

b. Osteoarthritis

c. Systemic Lupus Erythematosus

d. Ankylosing Spondylitis

b. Osteoarthritis

Osteoarthritis is not inflammatory because it lacks

a. Rubor

b. Calor

c. Palor

d. a and b

e. b and c

f. All

d. a and b

Rheumatologic disorder:

Autoimmune disease that affect women more than men more commonly known as lupus.

a. Rheumatoid Arthritis (RA)

b. Osteoarthritis

c. Systemic Lupus Erythematosus

d. Ankylosing Spondylitis

c. Systemic Lupus Erythematosus

Systemic Lupus Erythematosus causes the following.

a. Butterfly-shaped rash or Malar rash in the face

b. Photosensitivity

c. Most common renal complications like nephritis

d. a and b

e. b and c

f. All

f. All

Rheumatologic disorder:

Autoimmune disease that usually affects the spinal column of the patient.

a. Rheumatoid Arthritis (RA)

b. Osteoarthritis

c. Systemic Lupus Erythematosus

d. Ankylosing Spondylitis

d. Ankylosing Spondylitis

Ankylosing Spondylitis except:

a. Affects men more than women

b. Characterized as fusion of the spine or more commonly describe as Bamboo spine

c. Manifested as Enthesitis: Inflammation of the enthesis

d. Manifested as Sacrolitis: Inflammation of sacroiliac joint

e. None

e. None

Autoimmune disease except:

a. Rheumatoid Arthritis (RA)

b. Osteoarthritis

c. Systemic Lupus Erythematosus

d. Ankylosing Spondylitis

e. None

b. Osteoarthritis - not autoimmune, not inflammatory

Manifested as enthesitis, and sacrolitis.

a. Rheumatoid Arthritis (RA)

b. Osteoarthritis

c. Systemic Lupus Erythematosus

d. Ankylosing Spondylitis

d. Ankylosing Spondylitis

Analgesics

a. Drugs that are used to induce analgesia

b. Can be Non-Narcotics and Narcotic Analgesics

c. Both

d. None

c. Both

Non-Narcotics

a. Does not cause narcosis

b. p-nitrophenol Derivatives

c. NSAIDs

d. a and b

e. a and c

f. All

e. a and c

Non-Narcotics

a) Does not cause narcosis

b) p-aminophenol Derivatives

c) NSAIDs

Acetaminophen or paracetamol

a. Weak prostaglandin inhibitor in periphery; Weak cyclooxygenase inhibitor

b. Has analgesic & antipyretic activity; lacks anti-inflammatory

c. Can cause hepatotoxicity

d. a and b

e. b and c

f. All

f. All

Acetaminophen or paracetamol uses:

a. 1st line agent for osteoarthritis due to relative safety b. Aspirin substitute for patient with Aspirin effects intolerance

c. They are safe for pregnant women, lactating women and children

d. a and b

e. b and c

f. All

f. All

1st line agent for osteoarthritis.

a. Paracetamol

b. Aspirin

c. Ibuprofen

d. Indomethacin

e. Sulindac

a. Paracetamol

Risk factor for hepatotoxicity by paracetamol.

a. Higher dose intake than recommended dose; >5mg/kg/day

b. Pre-existing liver disease

c. Concomitant use of CYP1A2 inducers

d. a and b

e. b and c

f. All

f. All

NSAIDs except:

a. Non-steroidal Anti-Inflammatory Drugs

b. Does not possess Cyclopentanoperhydrophenanthrenes (CPPP) nucleus found in steroidal drugs

c. Anti-inflammatory drug due to its mechanism

d. Chemically weak organic acids

e. None

e. None

Only NSAID that is not a weak organic acid but instead, a prodrug converted to acetic acid derivative.

a. Nabumetone

b. Ibuprofen

c. Indomethacin

d. Naproxen

e. Aspirin

a. Nabumetone

Facilitate conversion of arachidonic acid into prostanoids.

a. Cyclooxygenase (COX)

b. Peroxidase (POX)

c. Both

d. None

c. Both

Convert arachidonic acid to PGG2.

a. Cyclooxygenase (COX)

b. Peroxidase (POX)

c. Both

d. None

a. Cyclooxygenase (COX)

Convert PGG2 acid to PGH2.

a. Cyclooxygenase (COX)

b. Peroxidase (POX)

c. Both

d. None

b. Peroxidase (POX)

COX-1

a. Constitutive Enzymes

b. PGs for homeostatic functions

c. Important for gastroprotection and renal vasodilation for enhance renal clearance

d. a and b

e. b and c

f. All

f. All

COX-2

a. Inducible Enzymes

b. Triggered due to certain adverse stimulus like microbial invasion and physical injury

c. Responsible for producing prostaglandins for inflammation which is PGE2

d. a and b

e. b and c

f. All

f. All

True statements.

a. Majority of NSAIDs are non-selective COX inhibitors

b. Some NSAIDs block COX-1 more than COX-2

c. Selective COX-1 inhibitor NSAIDs are safer for the stomach

d. a and b

e. b and c

f. All

d. a and b

Selective COX-2 inhibitor NSAIDs are safer for the stomach

Non-selective COX inhibitor

I. Aspirin

II. Pyrazolones derivatives

III. Indole derivatives

IV. Pyrole alkalonic acid derivatives

V. Phenylacetic acid derivatives

VI. Fenamates

VII. Oxicam derivatives

VIII. Propionic acid derivatives

a. I, II, III, IV, V, VI, VII, VIII

b. I, II, III, IV, V, VI,

c. III, IV, V, VI, VII, VIII

d. I, II, III, IV, V,

e. I, II, VII, VIII

a. I, II, III, IV, V, VI, VII, VIII

The only irreversible COX inhibitor.

a. Phenylbutazone

b. Indomethacin

c. Tolmetin

d. Aspirin

d. Aspirin

NSAID prototype.

a. Phenylbutazone

b. Indomethacin

c. Tolmetin

d. Aspirin

d. Aspirin

Aspirin pharmacologic effects except:

a. Analgesic

b. Anti-inflammatory

c. Antipyretic

d. Antiplatelet

e. Anticancer

f. None

f. None

Aspirin at <600mg/day

a. Analgesic

b. Central mechanism: Inhibits pain perception at subcortical sites

c. Peripheral mechanism: Irreversible COX inhibitor

d. a and b

e. b and c

f. All

f. All

Aspirin at 3.2-4.0 g/day

a. Anti-inflammatory

b. Peripheral mechanism: irreversible COX inhibitor

c. Both

d. None

c. Both

Aspirin at 0.3 -1.2 g/day except:

a. Antipyretic

b. Central mechanism: Inhibits response to interleukin-1

c. Block of endogenous pyrogen, IL-1, leading to ↓Body temperature

d. Peripheral mechanism: irreversible COX inhibitor

e. Causes cutaneous vasodilation

f. None

f. None

Aspirin at NMT 325 mg/day

a. Antiplatelet

b. TXA2 synthesis inhibition

c. Clotting

d. a and b

e. b and c

f. All

d. a and b

Aspirin at NMT 325 mg/day

a) Antiplatelet

b) TXA2 synthesis inhibition - a potent aggregator

c) Bleeding

Aspirin potential use in cancer is attributed to

a. Chronic inflammation associated to overexpression of COX-2

b. Chronic inflammation associated to overexpression of COX-1

c. Acute inflammation associated to overexpression of COX-2

d. Acute inflammation associated to overexpression of COX-1

e. None

a. Chronic inflammation associated to overexpression of COX-2

Aspirin toxicities

a. Gastritis and gastrointestinal ulcer bleeding

b. Decrease in Glomerular Filtration Rate

c. Both

d. None

c. Both

Gastritis and gastrointestinal ulcer bleeding

- Related to its COX-1 inhibition property resulting to negative alteration of cytoprotection

- treated with Proton pump inhibitors (PPIs): 1st line agents for inhibition of hydrochloric acid

- formerly treated with Misoprostol: alternative but was already banned due to its abortifacient effect

Glomerular Filtration Rate (GFR)

- Alteration in prostaglandins

- Prostaglandin made by COX-1 is important for renal vasodilation which is essential in ↑ GFR

- Aspirin then ↓ Prostaglandin level needed for renal vasodilation resulting to ↓ GFR

Aspirin toxicities except:

a. Hypersensitivity Reactions

b. Uricosurics agonism

c. CNS toxicity

d. Reye's Syndrome

e. None

b. Uricosurics agonism - should be urucosurics ANTAGONISM.

Hypersensitivity reactions by Aspirin.

a. NSAID-induced Bronchial Asthma

b. ASA Hypersensitivity Syndrome

c. Both

d. None

c. Both

Hypersensitivity reactions by Aspirin cause by more activation of LOX because of inhibition of COX.

a. NSAID-induced Bronchial Asthma

b. ASA Hypersensitivity Syndrome

c. Both

d. None

a. NSAID-induced Bronchial Asthma

Hypersensitivity reactions by Aspirin manifested as nasal polyposis & chronic sinusitis.

a. NSAID-induced Bronchial Asthma

b. ASA Hypersensitivity Syndrome

c. Both

d. None

b. ASA Hypersensitivity Syndrome

Antagonized uricosuric effect of uricosurics.

a. Aspirin

b. Tolmetin

c. Salicylates

d. a and b

e. b and c

f. All

f. All

Aspirin dose that can decrease renal excretion of urate.

a. <5 g/day

b. <4 g/day

c. <3 g/day

d. <2 g/day

d. <2 g/day

Aspirin is contraindicated to gout patients taking urocosurics.

a. True

b. False

a. True

Mild CNS effects of aspirin.

a. Salicylism

b. Acid-base imbalances, Hallucinations

c. Respiratory depression

a. Salicylism

Manifestations of Salicylism.

a. Hyperthermia

b. Tinnitus

c. Hyperventilation

d. a and b

e. b and c

f. All

f. All

Severe CNS effects of aspirin.

a. Salicylism

b. Acid-base imbalances, Hallucinations

c. Respiratory depression

b. Acid-base imbalances, Hallucinations

Fatal CNS effects of aspirin.

a. Salicylism

b. Acid-base imbalances, Hallucinations

c. Respiratory depression

c. Respiratory depression

Observed in children taking aspirin with fever & viral infection.

a. Salicylism

b. Acid-base imbalances, Hallucinations

c. Respiratory depression

d. Reye's Syndrome

d. Reye's Syndrome

Fatal complications of Reye's Syndrome by aspirin.

a. Hepatic Failure

b. Encephalopathy

c. Both

d. None

c. Both

Pyrazolone derivatives

a. Phenylbutazone

b. Dipyrone

c. Sulfinpyrazone

d. a and b

e. b and c

f. All

f. All

Pyrazolone derivative that is not an NSAID but a uricosuric agent.

a. Phenylbutazone

b. Dipyrone

c. Sulfinpyrazone

d. a and b

e. b and c

f. All

c. Sulfinpyrazone

Pyrazolone derivatives.

a. Analgesic

b. Anti-inflammatory

c. No longer clinically impactful due to certain hematologic and nephro toxicities

d. a and b

e. b and c

f. All

f. All

Pyrazolone derivative hematologic toxicities.

a. Thrombocytopenia (↓ Platelet count)

b. Aplastic Anemia (↓ Platelet count, ↓ RBC, ↓ WBC)

c. Agranulocytosis (↓ Granulocyte count: Basophils, Eosinophils, Neutrophils)

d. a and b

e. b and c

f. All

f. All

Pyrazolone derivative nephrotoxicities.

a. Acute Tubular Necrosis

b. Anasarca

c. Nephrotic Syndrome

d. a and b

e. b and c

f. All

f. All

Indole derivatives except:

a. Indomethacin

b. Blocks COX-1 > COX-2

c. Can cause gastric effects at a higher extent than other NSAIDs

d. a and b

e. b and c

f. None

f. None

Uses of indomethacin

a. To enhance closure of Patent Ductus Arteriosus

b. Management of Bartter Syndrome

c. Treatment of pain in acute gout

d. a and b

e. b and c

f. All

f. All

Used to enhance closure of Patent Ductus Arteriosus.

a. Indomethacin

b. Aspirin

c. Nabumetone

d. Sulindac

a. Indomethacin

Management of Bartter Syndrome

Treatment of pain in acute gout

a. Indomethacin

b. Aspirin

c. Nabumetone

d. Sulindac

a. Indomethacin

Pyrrole alklanoic acid derivative.

a. Indomethacin

b. Tolmetin

c. Sulindac

d. Mefenamic Acid

b. Tolmetin

Phenylacetic acid derivatives

I. Sulindac

II. Alclofenac

III. Diclofenac

IV. Ketorolac

V. Etodolac

VI. Nabumetone

a. I, II, III, IV, V, VI

b. I, II, III

c. IV, V, VI

d. I, II, III, IV, V

e. II, III, IV, V, VI

a. I, II, III, IV, V, VI

Phenylacetic acid referred to as the true phenylacetates.

I. Sulindac

II. Alclofenac

III. Diclofenac

IV. Ketorolac

V. Etodolac

VI. Nabumetone

a. I, II, III, IV, V, VI

b. I, II, III

c. IV, V, VI

d. I, II, III, IV, V

e. II, III, IV, V, VI

b. I, II, III

Acetic acid derivatives.

I. Sulindac

II. Alclofenac

III. Diclofenac

IV. Ketorolac

V. Etodolac

VI. Nabumetone

a. I, II, III, IV, V, VI

b. I, II, III

c. IV, V, VI

d. I, II, III, IV, V

e. II, III, IV, V, VI

c. IV, V, VI

Can cause Steven Johnson Syndrome and Toxic Epidermal Necrolysis

a. Sulindac

b. Alclofenac

c. Diclofenac

d. Ketorolac

e. Etodolac

f. Nabumetone

a. Sulindac

Can be used as treatment for pain after surgery (Especially when anaesthesia effect has worn off).

a. Sulindac

b. Alclofenac

c. Diclofenac

d. Ketorolac

e. Etodolac

f. Nabumetone

d. Ketorolac

Fenamates.

a. Mefenamic Acid

b. Meclofenamic Acid

c. Flufenamic Acid

d. a and b

e. b and c

f. All

f. All

Fenamates.

a. Analgesic

b. Anti-inflammatory

c. Antipyretic

d. a and b

e. b and c

f. All

a. Analgesic

Should never be given to children.

a. Mefenamic acid

b. Ibuprofen

c. Paracetamol

d. Ketorolac

e. Aspirin

a. Mefenamic acid - Fenamates should never be given to children.

Safest NSAID to children.

a. Mefenamic acid

b. Ibuprofen

c. Paracetamol

d. Ketorolac

e. Aspirin

b. Ibuprofen

Oxicam derivatives

a. Piroxicam

b. Can cause bleeding and ulceration

c. Block COX-1 in greater extent than COX-2

d. a and b

e. b and c

f. All

f. All

Propionic acid derivatives

a. Analgesic

b. Anti-inflammatory

c. Antipyretic

d. a and b

e. b and c

f. All

d. a and b - Propionic acid derivatives are not antipyretic except ibuprofen and naproxen.

Used in Fever of Malignancy in which it can be used as a confirmatory agent if patient has cancer.

a. Ibuprofen

b. Naproxen

c. Ketoprofen

d. Flubiprofen

b. Naproxen

When patient has fever, patient is not responsive to 1st line antipyretics like Aspirin or Acetaminophen but is sensitive to Naproxen

Specific COX-2 inhibitors

a. Less associated to gastric effects like gastritis and gastrointestinal ulcer bleeding

b. Increased risk of acute thrombotic events to patient with cardiovascular problems

c. May lead to myocardial infarction and stroke

d. a and b

e. b and c

f. All

f. All

Specific COX-2 inhibitors except:

a. Celecoxib

b. Etoricoxib

c. Valdecoxib

d. Rofecoxib

e. None

e. None

Specific COX-2 inhibitors already withdrawn from the market due to toxic effects.

a. Celecoxib

b. Etoricoxib

c. Valdecoxib

d. Rofecoxib

e. a and b

f. c and d

f. c and d