8.1 - Anti-Inflammatories, Antipyretics, and Analgesics Flashcards
What cells release histamine? What does it do?
Released my mast cells
–> Histamine results in bronchoconstriction, vasodilation and increased vascular permeability, rhinitis & rhinorrhea
What are H1 receptor antagonists used for?
Antihistamines are used to reduce the effects of histamine to control mild allergic reactions
What kind of medication are diphenhydramine and desloratadine? What are they used for?
H1 Receptor Antagonist
–>Moderate anti-inflammatory effect
–> nasal vasoconstriction
What kind of drug is dimenhydrinate? What is it used for?
H1 Receptor antagonist
–> Used to reduce nausea and motion sickness
What are the adverse effects of H1 receptor antagonists like diphenhydramine, desloratadine, and dimenhydrinate?
–> Sedation
–> Xerostomia (d/t anti-muscarinic effects)
What are the body’s two responses to stress?
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)
What kind of medication is prednisone and betamethasone? What is its use?
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
What are the clinical uses for prednisone and betamethasone?
Suppress immunological response and inflammation
Respiratory diseases, rheumatoid arthritis, lupus, IBD, autoimmune diseases
Skin condition, fetal lung development (surfactant), adjunct to chemotherapy
What are the adverse effects of glucocorticoids?
–> 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
What kind of drugs are fluticasone, mometasone, budesonide?
Glucocorticoids used to treat chronic respiration in the respiratory system
What is salbutamol? What is it used for?
B2 agonist (short acting)
What kind of drugs are formoterol and salmeterol?
Long acting B2-agonists used in combination with glucocorticoids for asthma treatment.
What kind of drug is tiotropium? What is it used for?
Long acting muscle antagonist, bronchodilator
What is Reye’s syndrome?
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
What kinds of medication are ibuprofen, naproxen, and diclofenac?
NSAIDs
–> inhibit both COX1&2 and has Anti-inflammatory, analgesia, sometimes antipyretic
–> Less antiplatelet effects than ASA
What kind of medication is celecoxib?
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.
What kind of medication is acetaminophen?
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
How do you treat acetaminophen overdose?
The antidote is N-acetylcysteine (asap, ideally within 8 hours)
What are the three stages of perception of pain?
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)
How do NSAIDs reduce pain?
Reducing levels of prostaglandins that sensitize pain detectors in tissues
–> Useful for mild to moderate main, especially where there is inflammation
What kind of medication is morphine? What are its routes and dosing frequencies? Adverse effects?
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
Codeine:
Relationship to hepatic enzymes?
Strengths and use?
Converted to morphine by CYP 2D6
–> Weaker analgesic, effective antitussive
–> Often combined with acetaminophen and caffeine (T1-4)
Meperidine
–> Strength and dose?
Short term use only, give at 10x dose of morphine
Oxycodone
–> Dose, route?
2/3 morphine dose (p.o)
–> Often combined with acetaminophen
Hydromorphone
–> Route, dose?
Dilaudid (p.o., s.c., i.m., i.v)
–> 1/5 morphine dose
Fentanyl
–> Dose and route?
Transdermal
–> ~1/100 morphine dose
Loperamide
–> Use?
Antidiarrheal opioid with no effect on brain
Methadone
–> half life, use?
Very long half life, 1-2 days
–> Used to eliminate the euphoria associated with heroin and to reduce withdrawal in opioid use disorder
What kind of drug is an opioid antagonist?
Naloxone
–> treats opioid OD
What is a combination of buprenorphine and naloxone used for?
Buprenorphine is a partial agonist that prevents withdrawal, this combo is used to treat opioid use disorder
What kind of drugs are benzocaine, bupivacaine and lidocaine?
Local Anesthetics
–> Suppress pain by blocking conduction along axons (block voltage sensitive sodium channels)
Why are local anesthetics like benzocaine, lidocaine, and bupivacaine usually not given IV?
There is an increased risk of anti-arrhythmic effect
What are the adverse effects of local anesthetics like benzocaine, lidocaine, and bupivacaine?
–> 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
What are gabapentin, pregablin, and amitriptyline used for?
treatment of neuropathic pain - such as shingles
What are the adverse effects of gabapentin and pregablin?
Drowsiness and dizziness.
