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Pharma > Antihistamines > Flashcards

Antihistamines Flashcards

0
Q

Cyclizine

A

H1 antihistamine

First Generation Antihistamine

SLIGHT Sedation

Used in MOTION SICKNESS/Emesis

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1
Q

Cetirizine

A

H1 antihistamine

Second Generation antihistamine

Highly selective for H1 sites

Few anti-cholinergic side effects

Penetrate poorly into CNS, reducing sedative effects

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2
Q

Dimenhydrinate

A

First Generation Antihistamine

HIGH SEDATION effect

Used to treat motion sickness

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3
Q

Diphenhydramine

A

First Generation Antihistamine

HIGH SEDATION

USED to treat MOTION SICKNESS
Used in Non-H1 effects for LOCAL ANESTHESIA

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4
Q

Fexofenadine

A

H1 Antihistamine

Second Generation antihistamine

LOW SEDATION

  • highly selective for H1 sites and have few anti-cholinergic side effects
  • Penetrate poorly into CNS, reducing sedative effects
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5
Q

Loratadine

A

H1 antihistamine

Second Generation antihistamine

LOW Sedation

  • High selectivity for H1 sites and have few anti-cholinergic side effects
  • Penetrate poorly into the CNS, reduce sedative effects
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6
Q

Promethazine

A

H1 antihistamine

Used in treatment of Motion sickness/emesis
- Very Effective

Used as local anesthetic by BLOCKING SODIUM CHANNELS

Causes SEDATION
- Used as antiemetic

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7
Q

Adalimumab

A

Anti-TNF alpha

HUMAN antibody to TNF alpha

  • Mechanism: binds TNF to prevent interaction with receptor
    • Reduces circulating and localized levels of TNF

Application:

  • Inflammatory disease involving TNF
    • Parenteral Administration required
    • Rh ART, used in COMBO with METHOTREXATE
      • Elevated TNF in joints
    • Crohn’s disease, used in COMBO with AZATHIOPRINE
      • Elevated TNF in stool

Complications
- Increased frequency of infections (upper respiratory, urinary)

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8
Q

Etanercept

A

Anti-TNF agent

Fusion protein containing:

  • Ligand binding domain of TNF receptor
  • and Fc domain of IgG

Mechanism:
- Bind to TNF alpha binding domain to prevent interaction with receptor

Applications:

  • Parenteral administration required
  • Rh arthritis, used in combo with methotrexate
  • Crohn’s disease, used in combo with azathioprine

Complications:
- increased frequency of infections (upper respiratory, urinary)

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9
Q

Infliximab

A

Anti-TNF alpha agent

Humanized antibody to TNF

Binds to TNF alpha

  • Prevents interaction with receptor
  • reduces circulating and localized levels of TNF

Applications:

  • Parenteral administration required
  • Rh, used in combo with methotrexate
  • Crohn’s disease, used in combo with azathioprine

Complications
- Increased frequency of infections (upper respiratory, urinary)

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10
Q

Anakinra

A

Anti-IL-1 Agent

Competitive IL-1 R antagonist

Useful in treating Rh ART
- Possibly other inflammatory diseases

Short half life, daily injection required

Increased susceptibility to infection

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11
Q

Tofacitinib

A

Jak kinase inhibitor

Treatment in Rh ART

Administration: Oral

Second line treatment for Rh ART

Mechanism:

  • Inhibits all activity of cytokines required for adaptive immunity (IL-2, 4)
  • Inhibits activities of inflammatory cytokines: IL-

THERAPEUTIC DOSE: 5 mg bid (twice a day)
- Higher doses to produce potent immunosuppression AND adverse effects

Adverse effects:

  • Anemia, neutropenia, general myelosuppression
  • Increase risk of infection (herpes zoster)

Effect: Comparable to anti TNF in reducing active disease in Rh ART

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12
Q

Aspirin

A

Nonselective COX inhibitor

Prototypical NSAID inhibits COX-1 and COX-2

  • IRREVERSIBLY inhibits COX enzymes
  • Only NSAID with cardiovascular protective effects

Irreversibly inhibits COX-1 so no TXA2 for life of platelet (7-10 days)

Rapidly converted to salicylic acid
- Main portion of aspirin is acetyl group that acts as a acetyl group to permanently inhibit COX

All metabolites excreted in urine
- If elimination saturates beyond 600 mg, total body load and half life increase to 12-16 hours from 3-5

Selectivity (IC50): 4.4

  • IC50 is (COX-2/COX-1):
    - IC50 COX-1: 1.7
    - IC 50 COX-2: 7.5

Analgesic/antipyretic
Cardiovascular prophylaxis
- Due to reduced platelet aggregation

Intolerance:

  • SALICYLISM: Hypersensitivy to ASA
    • Hyperventilation, tinnitus, vertigo, emesis, sweating
  • Reye’s Syndrome: Associated with ASA and other salicylates used in children with viral illness
    • Acute encephalopathy, fatty liver degeneration
    • Associated with viral diseases and viral vaccines
Adverse effects:
- Dyspepsia: upper abdominal pain, bloating, nausea
    - 35% chronic NSAID users
- Ulcers
     - 16 % chronic NSAID users
     - Gastric more common than duodenal
     - Risk factors:
            - Greater than 65
            - High dose
            - Helicobacter pylori
            - Alcohol consumption
GI Bleeding

Prevention of Adverse effects:

  • H2 receptor antagonist
  • Proton pump inhibitor
  • MISOPROSTOL
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13
Q

Diclofenac

A

Nonselective COX inhibitor

Selectivity: 0.3
- Used in Rh ART

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14
Q

Diclofenac with Misoprostol

A

Nonselective COX inhibitor

Selective: 0.3
- Used in Rx arthritis and anti-inflammatory

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15
Q

Ibuprofen

A

Nonselective COX inhibitor

Selectivity: 2.6

16
Q

Indomethacin

A

Nonselective COX inhibitor

Selectivity: 10

Used in Rx arthritis/anti-inflammatory

High frequency of intolerance

17
Q

Ketorolac

A

Nonselective COX inhibitor

Selectivity: 395

Post-Surgical analgesic

18
Q

Naproxen

A

Nonselective COX inhibitor

Selectivity: 3.8

OTC analgesic/antipyretic

May have a safe profile than other NSAIDS (besides aspirin)

Can be used in Rx anti-inflammatory

Naproxen may ha

19
Q

Acetaminophen

A

Nonselective COX inhibitor

May be at risk for RENAL problems if taken
- Hepatotoxic at high doses

Activity is substantially reduced in presence of peroxides (often elevated at sites of inflammation)

  • Lacks effects on platelets, cardiovascular, and GI system
  • Analgesic and antipyretic effects equivalent to aspirin
20
Q

Celecoxib

A

COX-2 Selective Inhibitor

10-20 more times selective for COX-2 over COX-1

Reduced incidence of GI effects

Remains available despite ADVERSE EFFECTS of incresed event of cardiovascular events
- HTN, MI, Stroke

21
Q

Rofecoxib

A

COX-2 Selective NSAID

200 times more selective for COX-2 than COX-1

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