Principles Flashcards
What happens in phase 2 of metabolism?
The body adds another substance called glucuronic acid in a process known as conjugation which makes the drug water soluble and ready for excretion.
What are inducers of CYP450 enzyme?
- Rifampin
- Carbamazepine
- Phenobarbital
- Phenytoin
- Charcoal broiled foods
- Cabbage/Broccoli
- St. John’s Wort
What are inhibitors of CYP450 enzyme?
- Grapefruit Juice
- Erythromycin
- Cimetidine
- Ketoconazole
- Ritonavir
- Fluoxetine
- Paroxetine
What are examples of inhibitor drug interactions?
- Cimetidine and Warfarin
- Grapefruit Juice and Statins
What are the major hepatotoxic drugs?
- Tylenol
- Statins
- Isoniazid
- Methotrexate
- Amiodarone
What is affinity and how is it measured?
It is the strength of the binding relationship between a drug and its receptor, and it is measured by the equilibrium dissociation constant (Kd).
What is an agonist and what is an example of this?
Drugs that immediately activate a receptor and stimulates a response. Morphine is an example.
What is a partial agonist and what is an example of this?
Binds to the drug but produces a weaker response in comparison to a full agonist. Buprenorphine is an example.
What is a competitive antagonist and what is an example of this?
Drugs that compete with an agonist for the same receptor site. Narcan is an example.
What is tachyphylaxis and what is an example of this?
Occurs when the drug becomes less effective after repeated use over a short time, so the body quickly stops responding to it. Some nasal decongestants can cause this.
What are the three parts of the dose-response curve?
- Threshold dose: Smallest amount of drug that starts to produce a noticeable effect.
- Linear Phase: Middle part of the curve and is the “sweet spot” where the drug works efficiently.
- Maximal Effect: Top of the curve where the drug reaches its maximum effect.
What is additive effect and what is an example of this?
When two drugs with similar effects are taken together for a combined similar effect. Taking an ACE inhibitor and a diuretic will have an additive effect of lowering BP.
What is synergistic effect and what is an example of this?
When two drugs taken together produce a great effect than when taken by themselves. Aspirin and clopidogrel together have a much stronger effect of reducing heart attacks rather than when taken alone.
What is antagonistic effect and what is an example of this?
When one drug cancels out the effect of another. Beta blockers can cancel out beta agonists when taken together.
What is interference and what is an example of this?
When one drug affects how another drug is processed in the body. Antacids can interfere with the absorption of antibiotics like Tetracycline.