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IHO Week 5 AJL > Anti-inflammatory Drugs- Regal > Flashcards

Anti-inflammatory Drugs- Regal Flashcards

(41 cards)

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1
Q

Explain the general process of inflammatory process

A

Injury —-> Mediators —-> Inflammation: redness, swelling, heat, and pain

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2
Q

These cause redness/vasodilation

A

Histamine, PGE2, PGI2, kinins

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3
Q

These cause swelling/increased vascular permeability

A

Histamine, peptido leukotrienes (LTC4, LTD4, LTE4)

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4
Q

These cause pain

A

PGE, PGI, LTB4, kinins

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5
Q

These are chemotactic/direct migration of WBC

A

LTB4 (neutrophils, etc), peptido leukotrienes (eosinophils)

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6
Q

These cause fever

A

PGEs induce fever!

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7
Q

These cause airway constriction

A

histamine, peptido leukotrienes, kinins, PGD2

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8
Q

These cause hypotension

A

Kinins, histamine

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9
Q

What happens with oral administration of histamine?

A

Nothing, it’s inactivated by enzymes in the intestinal wall or liver after ingestion.

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10
Q

What happens with intracutaneous administration of histamine?

A

“Triple response” Itching, pain, wheal and flare

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11
Q

What causes (1) Localized redness (2) Flare (3) Localized edema or wheal formation?

A

(1) Arteriolar dilation
(2) nerves dilating neighboring arterioles
(3) Increased capillary permeability with leakage of the postcapillary venules

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12
Q

Symptoms of intranasal histamine?

A

Intense itching, sneezing, hypersecretion, nasal blockage

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13
Q

Symptoms of IV histamine?

A

Hypotension, tachycardia, broncoconstriction, flushing, headache, wheal and flare, stimulation of mucus secretion and gastric acid secretion

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14
Q

Stimulation of the H1 receptor causes what?

A 
Bronchoconstriction
Contraction of GI smooth muscle
Inc. capillary permeability (wheal) 
Pruritis (itch) and pain
Release of catecholamines from the adrenal medulla
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15
Q

Stimulation of the H2 receptor causes what?

A

Gastric acid secretion
Inhibition of IgE-mediated basophil histamine release
Inhibition of T lymphocyte mediated cytotoxicity
Suppression of Th2 cells and cytokines

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16
Q

Does first or second generation antihistamines have affinity for P-glycoprotein in the CNS?

A

Second generation has affinity for P-glycoprotein in CNS……Prob why the second generations are non-sedating…

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17
Q

What side effect did one of the first non-sedating antihistamine have that has now been fixed in the newer drugs?

Study These Flashcards
A

Cardiotoxicity with overdose

18
Q

What are the second generation antihistamines we need to know?

Study These Flashcards
A

Cetirizine (OTC)
Fexofenadine
Loratidine (OTC)

19
Q

What effect do the first gen antihistamines have that the second gens don’t?

Study These Flashcards
A

Second generation antihistamines don’t have any anticholinergic properties…..first gens have a little, but not as much as Atropine

20
Q 
Diphenhydramine (OTC)
MOA
ADME
TU and Common Side effects
Toxicities
Study These Flashcards
A

H1 antagonist (histamine)

A – good oral
D – widely, even CNS (no P-glycoprotein)
M – liver
E –urine

Ophthalmic solutions
Motion Sickness (Diph.)

Sedation, dry mouth, GI disturbances (anti-cholinergic action)

21
Q 
Chlorpheniramine 
MOA
ADME
TU and Common Side effects
Toxicities
Study These Flashcards
A

First generation – block H1, muscarinic, α-adrenergic, 5HT receptors

Ophthalmic solutions
Motion Sickness (Diph.)

Sedation, dry mouth, GI disturbances (anti-cholinergic action)

Suitable for day time use - ↓ sedation

22
Q

Cetirizine (Zyrtec) OTC
MOA
ADME
TU and Common Side effects

Study These Flashcards
A

H1 antagonist (histamine), Second generation

D - Able to cross BBB – have affinity for P-glycoprotein (efflux)

  • Less sedation than 1st generation (P-glyco)
  • Do NOT potentiate effects of CNS depressants
23
Q

Fexofenadine
MOA
ADME
TU and Common Side effects

Study These Flashcards
A

H1 antagonist (histamine), Second generation

D - Able to cross BBB – have affinity for P-glycoprotein (efflux)

  • Less sedation than 1st generation (P-glyco)
  • Do NOT potentiate effects of CNS depressants
24
Q

Loratadine [Claritin] (OTC)
MOA
ADME
TU and Common Side effects

Study These Flashcards
A

H1 antagonist (histamine), Second generation

D - Able to cross BBB – have affinity for P-glycoprotein (efflux)

  • Less sedation than 1st generation (P-glyco)
  • Do NOT potentiate effects of CNS depressants
25
``` Zileuton MOA ADME TU and Common Side effects Toxicities ```
Inhibits 5-LO (prevents synthesis of all leukotrienes) M – Cyp P450 Chronic asthma Drug interactions Monitor for hepatic toxicity
26
``` Zafirlukast MOA ADME TU and Common Side effects Toxicities ```
CysLTR1 (LTD/C/E4) receptor antagonists M – Cyp P450 Chronic asthma Montelukast used more due to once/day admin Drug-drug interactions
27
``` Montelukast MOA ADME TU and Common Side effects Toxicities ```
CysLTR1 (LTD/C/E4) receptor antagonists Chronic asthma Montelukast used more due to once/day admin
28
``` Acetylsalicylate (aspirin, OTC) MOA ADME TU and Common Side effects Toxicities ```
IRREVERSIBLY acetylates COX1 - GI ulceration (due to PG synthesis inhibition) - Secondary anemia - Prolonged gestation - ↓ Renal function - Abnormal Hepatic function - Increased bleeding time - Hypersensitivity-like reaction due to increased LT production (3-10% of asthmatics) - Reye Syndrome following viral infection in children
29
``` Ibuprofen [Advil] (OTC) MOA ADME TU and Common Side effects Toxicities ```
Inhibit both COX1 &2 A – oral D – good bioavailability – cross BBB; PPB E – glucuronidation; urine - GI ulceration (due to PG synthesis inhibition) - Secondary anemia - Prolonged gestation - ↓ Renal function - Abnormal Hepatic function - Increased bleeding time Fewer GI issues
30
``` Naproxen [Aleve] – long-acting ibuprofen (OTC) MOA ADME TU and Common Side effects Toxicities ```
Inhibit both COX1 &2 A – oral D – good bioavailability – cross BBB; PPB E – glucuronidation; urine - GI ulceration (due to PG synthesis inhibition) - Secondary anemia - Prolonged gestation - ↓ Renal function - Abnormal Hepatic function - Increased bleeding time Fewer GI issues
31
``` Ketorolac MOA ADME TU and Common Side effects Toxicities ```
Inhibit both COX1 &2 A – oral D – good bioavailability – cross BBB; PPB E – glucuronidation; urine - GI ulceration (due to PG synthesis inhibition) - Secondary anemia - Prolonged gestation - ↓ Renal function - Abnormal Hepatic function - Increased bleeding time Fewer GI issues
32
``` Indomethacin MOA ADME TU and Common Side effects Toxicities ```
Inhibit both COX1 &2 A – oral D – good bioavailability – cross BBB; PPB E – glucuronidation; urine - GI ulceration (due to PG synthesis inhibition) - Secondary anemia - Prolonged gestation - ↓ Renal function - Abnormal Hepatic function - Increased bleeding time
33
Ketorolac
Promoted primarily for analgesia but is also anti-inflammatory
34
Ketoprofen
ibuprofens goofy cousin......?
35
Sulindac
????
36
Piroxicam
Once a day administration....can cause dose related serious GI bleeding
37
Celecoxib MOA Uses Side effects
COX2 Inhibitor – theoretically beneficial since COX1 protects GI mucosa Safe in aspirin-hypersensitive individuals Thrombotic CV events with chronic use
38
``` Acetaminophen (Tylenol) OTC MOA ADME TU and Common Side effects Toxicities ```
Weak inhibitor of COX (esp. in brain); minimal anti-inflammatory effects.....antipyretic and analgesic A – oral D - ??? M – liver (Cyp P450) E – urine Toxic when used in conjunction with alcohol---> N-acetyl-p-benzo-quinone Tx: N-acetylcysteine
39
Kinin Inhibitors, C1IHN MOA TU and Common Side effects Toxicities
Inhibits kallikrein Nasal allergies, rhinitis associated with rhinoviral infections; dental pain Since Kinin, complement, coagulation, and fibrinolytic pathways have a interrelationship, perturbing one pathway disrupts another
40
Four key enzymes for kinin inhibitors?
Four key enzymes: HFa, C1 esterase, kallikrein, plasmin
41
Where do you find COX 1 and COX 2?
COX1 – platelets, other cells (protect GI mucosa) COX2 – Constitutively expressed in brain and kidney; induced in other tissues in response to inflammation

IHO Week 5 AJL (2 decks)

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