8.1 - Anti-Inflammatories, Antipyretics, and Analgesics

Question 1

What cells release histamine? What does it do?

Answer 1

Released my mast cells
–> Histamine results in bronchoconstriction, vasodilation and increased vascular permeability, rhinitis & rhinorrhea

Question 2

What are H1 receptor antagonists used for?

Answer 2

Antihistamines are used to reduce the effects of histamine to control mild allergic reactions

Question 3

What kind of medication are diphenhydramine and desloratadine? What are they used for?

Answer 3

H1 Receptor Antagonist
–>Moderate anti-inflammatory effect
–> nasal vasoconstriction

Question 4

What kind of drug is dimenhydrinate? What is it used for?

Answer 4

H1 Receptor antagonist
–> Used to reduce nausea and motion sickness

Question 5

What are the adverse effects of H1 receptor antagonists like diphenhydramine, desloratadine, and dimenhydrinate?

Answer 5

–> Sedation
–> Xerostomia (d/t anti-muscarinic effects)

Question 6

What are the body’s two responses to stress?

Answer 6

Sympathetic system (E) –> Short term response

Glucocorticoids (cortisol) –> Long-term response
(chronic stress leads to a lot of problems, similarly, longterm exposure to other glucocorticoids do too)

Question 7

What kind of medication is prednisone and betamethasone? What is its use?

Answer 7

Hydrocortisone (Glucocorticoids)
–> anti-inflammatory effects (through binding to glucocorticoid receptor)
–> Aldosterone like effects (Na/water retention and K secretion) through bindings to the mineralocorticoid receptor

Question 8

What are the clinical uses for prednisone and betamethasone?

Answer 8

Suppress immunological response and inflammation
Respiratory diseases, rheumatoid arthritis, lupus, IBD, autoimmune diseases
Skin condition, fetal lung development (surfactant), adjunct to chemotherapy

Question 9

What are the adverse effects of glucocorticoids?

Answer 9

–> Risk of infections
–> Slow wound healing
–> Increase BGL
–> Risk of hypertension
–> Protein catabolism - muscle atrophy, thinning of skin
–> Redistribution of adipose tissue (round face, at base of neck)
–> Osteroporosis
–> Euphoria, increased energy

Question 10

What kind of drugs are fluticasone, mometasone, budesonide?

Answer 10

Glucocorticoids used to treat chronic respiration in the respiratory system

Question 11

What is salbutamol? What is it used for?

Answer 11

B2 agonist (short acting)

Question 12

What kind of drugs are formoterol and salmeterol?

Answer 12

Long acting B2-agonists used in combination with glucocorticoids for asthma treatment.

Question 13

What kind of drug is tiotropium? What is it used for?

Answer 13

Long acting muscle antagonist, bronchodilator

Question 14

What is Reye’s syndrome?

Answer 14

A life threatening condition that occurs when ASA is given to children with viral infections
–> Encephalopathy w cerebral edema and massive lipid infiltration of the liver

Question 15

What kinds of medication are ibuprofen, naproxen, and diclofenac?

Answer 15

NSAIDs
–> inhibit both COX1&2 and has Anti-inflammatory, analgesia, sometimes antipyretic
–> Less antiplatelet effects than ASA

Question 16

What kind of medication is celecoxib?

Answer 16

COX-2 Inhibitors
–> Inhibits only COX2; it was thought that COX2 produced only harmful prostaglandins but is also produces kinds that improve kidney function and reduce risk of thrombosis

Most very specific COX2 inhibitors were pulled from the market d/t side effects.

Question 17

What kind of medication is acetaminophen?

Answer 17

Antipyretic/Analgesic
–> No anti-inflammatory or anti-platelet effect
–> Preferred to ASA d/t no GI, hematological, or hypersensitivity, or association with Reye’s syndrome.

OD with lead to hepatotoxicity or death

Question 18

How do you treat acetaminophen overdose?

Answer 18

The antidote is N-acetylcysteine (asap, ideally within 8 hours)

Question 19

What are the three stages of perception of pain?

Answer 19

Detection of pain by local receptors
–> Reduced by NSAIDS

Transmission of pain in the spinal cord
–> Reduced by local anesthetics

Transmission of pain to the brain
–> Reduced by opioids (derivatives of morphine, best for moderate to severe pain, similar to natural endorphins)

Question 20

How do NSAIDs reduce pain?

Answer 20

Reducing levels of prostaglandins that sensitize pain detectors in tissues
–> Useful for mild to moderate main, especially where there is inflammation

Question 21

What kind of medication is morphine? What are its routes and dosing frequencies? Adverse effects?

Answer 21

Mu Opioid Receptor Agonist
–> s.c., i.m., i.v., p.o w F = .35, q4h; also available as extended release p.o.

Adverse Effects
–> Drowsiness, mental clouding, nausea, hypotension, pruritis, resp depression that decrease with time
–> Constipation and miosis does not decrease over time
–> Tolerance and addiction

Question 22

Codeine:
Relationship to hepatic enzymes?
Strengths and use?

Answer 22

Converted to morphine by CYP 2D6
–> Weaker analgesic, effective antitussive
–> Often combined with acetaminophen and caffeine (T1-4)

Question 23

Meperidine
–> Strength and dose?

Answer 23

Short term use only, give at 10x dose of morphine

Question 24

Oxycodone
–> Dose, route?

Answer 24

2/3 morphine dose (p.o)
–> Often combined with acetaminophen

Question 25

Hydromorphone
–> Route, dose?

Answer 25

Dilaudid (p.o., s.c., i.m., i.v)
–> 1/5 morphine dose

Question 26

Fentanyl
–> Dose and route?

Answer 26

Transdermal
–> ~1/100 morphine dose

Question 27

Loperamide
–> Use?

Answer 27

Antidiarrheal opioid with no effect on brain

Question 28

Methadone
–> half life, use?

Answer 28

Very long half life, 1-2 days
–> Used to eliminate the euphoria associated with heroin and to reduce withdrawal in opioid use disorder

Question 29

What kind of drug is an opioid antagonist?

Answer 29

Naloxone
–> treats opioid OD

Question 30

What is a combination of buprenorphine and naloxone used for?

Answer 30

Buprenorphine is a partial agonist that prevents withdrawal, this combo is used to treat opioid use disorder

Question 31

What kind of drugs are benzocaine, bupivacaine and lidocaine?

Answer 31

Local Anesthetics
–> Suppress pain by blocking conduction along axons (block voltage sensitive sodium channels)

Question 32

Why are local anesthetics like benzocaine, lidocaine, and bupivacaine usually not given IV?

Answer 32

There is an increased risk of anti-arrhythmic effect

Question 33

What are the adverse effects of local anesthetics like benzocaine, lidocaine, and bupivacaine?

Answer 33

–> At high doses: bradycardia, cardiac arrest, resp depression
–> Low doses can lead to CNS excitability (seizures)
–> Can lead to increased levels of methemoglobin that is incapable of carrying oxygen

Question 34

What are gabapentin, pregablin, and amitriptyline used for?

Answer 34

treatment of neuropathic pain - such as shingles

Question 35

What are the adverse effects of gabapentin and pregablin?

Answer 35

Drowsiness and dizziness.