Clinical Activity (Sweatman) Flashcards
What the advantage of taking medicine with food vs. no food?
- what aspect of ADME is affected?
- Risk of Fatty Foods?
ABSORPTION - affected
Advantage:
- eating food with a pill reduces gastric irritation
Fatty Foods:
- Lipophilic drugs may not be absorbed well with fatty foods because they’ll stay with the food and get excreted
What is the major variable affected the distribution of a drug after it is given Intramuscularly or Subcutaneously?
Perfusion of the Site greatly affects what will happen to the drug after it is injected
**Neonates also have very different rates of perfusion
What drug is contraindicated with Carbamazepine (mood stabilizer) and why?
- classify this interaction
Clarithromycin and Carbamazepine BOTH are metabolized by CYP3A4
- COMPETITIVE inhibition takes place
- Carbamazepine gets out competed and toxicity can result
What group of antifungals are contraindicated with simvastin and Lovastatin?
- why?
- Which or these is the worst?
- What condition could mixing these drugs cause?
Azoles act on CYP3A4 as well
Worst —> Best:
- Voriconazole
- Itraconazole
- Fluconazole
Condition:
- Rhabdomylosis - Myoglobin in Kidneys
What are two major factors that affect Renal Tubule Secretion (RTS)?
- Competitive Inhibition
(e. g. Probenecid blocks Penicillin Excretion) - Are Tubules Damaged??
Cimetidine and Trimethoprim can act to block renal tubule secretion of what drugs?
- Pramipexol
- Dofetilide
What usually happens to a receptor when over-stimulated by a drug?
It gets down-regulated
What groups of drugs act at the ß2-receptor to upregulate its presence?
- which down regulates the receptor by its presence?
Coriticosteroids upregulate ß2-receptors
Opiates Downregulate ß2 receptors
What are some factors to consider when thinking about drug reabsorption in the distal tubule?
- Competitive Inhibition
2. pH in Renal Tubule
T or F: an acidic pH in the renal tubule can help cure Acetylsalacyclic Acid overdose
False, overly basic pH’s do this
You want a basic pH because this deprotonates the acid (making it charged) - charged ions are excreted in the distal tubule
- You might give the patient bicarb to do this
What are the two ways that a receptor can be agonized?
Directly
- Depends on duration of Ligand binding
Indirectly (drugs from a different class)
- Could Exhaust the Neurotransmitter that Needs to be used
- Could cause Off target effects
Why should you not eat leafy green vegetables while taking Warfarin?
- what about NSAIDs?
- Vegetables high in Vit. K are bad with Warfarin because Warfarin acts to prevent the action of Vit. K in making clotting proteins in the liver
- NO DO NOT TAKE NSAIDs with Warfarin
T or F: the relationship between Amoxicillin and Clavuanate is a not at receptor interaction
True, clavulanate prevents ß-lactamases from cleaving Amoxicillin
**PIP/TAZO relationship is the same deal
T or F: for fear of a competitive interaction you should avoid taking Simvastatin with Niacin.
False, this is a not at receptor interaction
- Both act to lower LDL in different ways
You are given and inhaled anesthetic before surgery. How will that drug leave your body?
- Will be exhaled
What is P-gp?
- what does it do?
- Where is it found?
P-gp = P-glycoprotein
Function:
- Energy Dependent Drug Efflux Pump
Where:
- Found at any tissue barrier
What happens if you foods containing lots of Tyramine while taking an MAOI?
You can get Tyramine overdose because Tyramine is acted on by MonoAmine Oxidase
Why would you give a vasocontricting agent with a local anesthetics?
- Vasoconstriction keeps the Drug from Spreading out (localized)
What will a neutral pH created by an antacid do the the absorption of acidic compounds in the stomach?
- Neutral pH will hinder absorption because acids need to be protonated to travel through stomach epithelium
What happens if you try to chew up an enterically coated drug?
The drug will get broken down and made ineffective in the stomach or it will get released at the inappropriate time
What’s the effect of taking a laxative with another drug?
The other drug may be expelled too fast to reach maximal efficacy
What should you not use to take you tetracyclines with?
- why?
Milk - tetracycline chelates the calcium rendering it ineffective (it also chelates calcium in bone etc.)
T or F: grapefruit juice has a huge tendency to change activity of drugs.
True, because components in it act on CYPs
What herpes drugs are actually activated by 1st pass metabolism?
- what is the advantage of giving them as a prod-drug
Vancyclovir
Valganciclovir
Prodrug Advantage - allows for increased absorption
Most drugs have a large therapeutic window. What 3 drugs did Sweatman tell have narrow therapeutic windows?
- Caramazepine
- Cyclosporine
- Digoxin
- Ethosuximide
Which is quicker enzyme induction or enzyme inhibition?
- why?
Enzyme Inhibition is much quicker
- Enzyme induction requires the synthesis of proteins which is time consuming
What is the issue with taking cyclosporin and tacrolimus with a kidney transplant?
They can cause loss of the transplant due to drug toxicity since they are metabolized by the liver
In what situation would you definitely need to administer a chelating agent?
- In the case of heavy metal ingestion
Go Back on Look at His Mind Map
- lots of stuff not included in these FC’s
Go Back on Look at His Mind Map
- lots of stuff not included in these FC’s
What things factor into Phamacokinetic metabolism?
- Pharmacodynamic?
Pharmacokinetic
- Absorption
- Distribution
- Metabolism
- Excretion
Pharmacodynamic
- Additive
- Synergistic
- Antagonistic
T or F: affecting the the rate absorption is extremely clinically significant.
False, changing the EXTENT of absorption is more important clinically
Why would you need to be more conscious of dosing with a drug like warfarin with older people and newborns?
- Older people and newborns have variable plasma protein levels
What factor should be considered the most when determining whether plasma protein will play an important role in the distribution of a drug?
**How much drug there is relative to the Plasma Protein
**Way more drug than plasma protein binding sites, then affects aren’t that significant
**Way less drug than binding sites then a change in binding can become very significant
T or F: it takes a long time to build up a drug in adipose tissue and it takes a long time to get it back out
True
What effect does induction typically have on drugs?
- what phase of metabolism is typically involved in induction?
It shortens the drug half life
Phase II
