study day 8

Question 1

histamine

mechanism of action

Answer 1

Histamine release from mast cells
triggered by interactions between an allergen and mast cell IgE antibodies

Question 2

anthistamines

use, examples, adverse

Answer 2

antihistamines= H1 receptor antagonists
reduce Bronchoconstriction, vasodilation and increased vascular permeability

Diphenhydramine (benadryl), desloratadine (aerius)
- Useful effects:
1) Moderateanti-inflammatory effect
2) Nasal vasoconstriction

Dimenhydrinate (gravol) is also used to reduce nausea and motion sickness

Adverse effects (anti muscarinic) :
1) Sedation, xerostomia (drymouth)
2) Anti sludge ,dehydration

Question 3

glucocorticoids

Answer 3

Very powerful inflammation reducing agents
- Responsible for the negative effects of long term stress- suppressing of immune system

• In response to stress the body activates
  1) Sympathetic system (adrenaline): short term response
  2) Glucocorticoids (cortisol) :long term response

prednisone, betamethasone
- structure greatly resembles that of aldosterone
- demonstrates anti-inflammatory effects (by binding the glucocorticoid receptor)
- aldosterone like effects such as Na+/ water
retention and K+ secretion (by binding the mineralocorticoid receptor)

Question 4

clinical use of coirticoids and adverse effects

Answer 4

Suppress the immunological response and reduce inflammation
- Used for rheumatoid arthritis, lupus, inflammatory bowel disease,
autoimmune disease (major inflammatory diseases)
- Other uses:
1) skin conditions (psoriasis), fetal lung development, with chemotherapy (often given with chemo as i gives a boost in energy but also treats nausea)

Adverse effects: especially long term
- Increased risk of infections
- Slow wound healing
- hyperglycemia
- hypertension
- Protein catabolism (muscle atrophy, thinning of skin)
- Redistribution of adipose tissue (round face, buffalo hump)

Question 5

drugs used in chronic inflammation of resp system

Answer 5

1) glucorticoids –> Fluticasone, mometasone, budesonide

Leukotriene antagonists (leukotrienes= contraction of the bronchi= asthma symptoms)
1) Montelukast (singulair)
1) Salbutamol
2)Tiotropium
- Drugs used in the treatment of asthma are often available as combinations
of glucocorticoids and long-acting bronchodilators
1) budesonide/formoterol
2) fluticasone/salmeterol
often given together

Question 6

NSAIDs

action, example, adverse, overdose

Answer 6

Mechanism of action:
- Inhibit cyclo-oxygenases (COX) enzymes that produce thromboxane A2 (pro-aggregation) and prostaglandins (pain, inflammation, fever)

Acetylsalicylic acid→
decreased platelet aggregation, fever, pain)
1) Anti platelet effects
2) Anti-inflammatoryeffects
3) Anti pyretic effects
4) Analgesic effects

Adverse effects
1) Gastrointestinal irritation, gastric ulcers
2) Prolonged bleeding time
3) Renal insufficiency,
4) Na+ and water retention
4) hypersensitivity reaction

overdose:
- Tinnitus (ringing ears), metabolic acidosis, hyperventilation, reye’s syndrome in children
- Reye’s syndrome: may produce acute childhood encephalopathy with cerebral edema and massive hepatic steatosis (lipid infiltration of the liver)

Question 7

other NSAIDS

Answer 7

Other NSAIDs→
Ibuprofen, naproxen, diclofenac they all inhibit the two different cyclooxygenases to a certain
degree)
- Main uses: anti-inflammatory, analgesic, sometimes antipyretic
- Less antiplatelet effects than ASA

Question 8

COX-2 inhibitors and Acetominephen

Answer 8

Celecoxib (Celebrex)
- NSAIDs inhibit both cyclo-oxygenases (COX 1 and COX 2)
- produces prostaglandins that improve kidney function and reduce risk of thrombosis

Acetaminophen (tylenol)
- Generally preferred to ASA (less toxic)
- No gastro-intestinal or hematological effects of hypersensitivity reactions
- No association with reye’s syndrome
- overdose= hepatotoxicity, death

Question 9

analgesic drugs

Answer 9

Perception of pain involves three stages:
1)Detection of pain in tissues by specialized local pain receptors
2)Transmission of pain to the spinal cord
3)Transmission of pain to the brain

• Local anesthetics block sodium channels= block transmission of electrical signal of pain
• NSADIs reduce pain by reducing levels of prostaglandins that sensitize pain detectors in tissues
• NSAIDs are useful for mild to moderate pain (especially when there is inflammation)
• Narcotics (opioid) drugs inhibit the transmission of pain from the spinal cord to the brain
• Uses: moderate to severe pain

Question 10

morphine

Answer 10

morphine
- Mu opioid receptor agonist
- Adverse effects
1) drowsiness/mental clouding
2) Constipation
3) Miosis
4) Hypotension
5) Pruritus
6) Respiratory depression

At the beginning of tx people tend to be confused and have adverse effects leading to altered living but it goes away over time

Question 11

other opiods

Answer 11

Codeine (pro drug)
- Converted to morphine in the body by CYP2D6
- Weaker analgesic

Meperidine (demerol)
- Short-term use only;
- dose= 10x morphine dose

Oxycodone
- P.o
- 2⁄3 morphine dose

Hydromorphone (dilaudid)
- 1⁄5 morphine dose

Loperamide
- Antidiarrheal (no effect on the brain)
- (morphine that only has the constipating effect)

Methadone
- Very long half life
- used to eliminate the euphoria associated with heroin and help treat opioid addiction
- Prevents someone from getting the high because the receptor is already occupied

Naloxone
- To treat opioid overdose