The study of how various dosage forms influence the way in which a drug affects the body
What is Pharmaceutics?
Enteral (oral, Sublingual/Buccal, Suppositories; varying bioavailability)
Parenteral (injection;100% bioavailable)
Other (Eye drops, Inhalers, etc; varying bioavailability)
What are the types of absorption routes?
Occurs after the drug is absorbed into the bloodstream
What is distribution?
What is metabolism?
elimination of hydrophilic drugs from the body via the kidneys
What is elimination?
Determinant of how a drug dissolutes
What is dosage form?
What are the influences of oral drug bioavailability?
Non-polar Lipophilic drugs are easily distributed into fatty tissue and can cross BBB and placenta
Polar Hydrophilic typically remain in highly vascularized spaces and are easily eliminated via urine
What is permeability of cell membrane?
Liver enzymes that target substrates that are lipophilic non-polar and covert them to hydrophilic polar form
Known as "The filter"
Serum Creatinine (🫐0.6-1.2mg/dL 🎀0.5-1.1mg/dL)
BUN (8-20mg/dL)
Urine Output (>30ml/hr)
Creatinine Clearance (CrCl) & Estimated Glomerular Filtration Rate (eGFR) = 90-120ml/min
What is the Glomerulus and normal lab values for kidney function?
The study of what the body does to the drug (ADME).
Whats is Pharmacokinetics?
- Age (Neonates and Elders have a high pH)
- Time of Day (pH is lowest when we wake up)
- Presence of food
- Tums/Medications
- Diseases/Conditions
Albumin is the most common blood protein; when drug is bound to this protein, it is a highly-bound drug/inactive so it stays in the bloodstream (Phenytoin is 🗝️)
Free drugs are active drugs that are not bound to albumin and can leave the bloodstream so they can reach extravascular tissue and intended target
What is Protein Binding?
PS-PORCS
Phenytoin, Smoking, Phenobarbital, Oxcarbazepine, Rifampin, Carbamazepine, St. John's Wort
What are components that induce metabolism?
Elevated serum creatinine, and BUN with decreased CrCl, eGFR, and urine output
The percentage of how much active drug reaches and is absorbed into the bloodstream
What is bioavailability?
Grapefruit inhibits it's function and specifically does not fair well with Statins which results in rapid muscle breakdown (rhabdomyolysis) if taken together
Competition leads to toxicity and albumin deficiency can lead to more free drug levels causing respiratory distress.
What are complications of Highly-Bound Drugs?
PACMAN ♡ Grapefruit
Protease inhibitor (HIV), Azole antifungal (fluconazole, ketoconazole), Cimetidine (H2RAs), Macrolides (ACE, Azithromycin, Clarithromycin, Erythromycin), Amiodarone, Non-DHP Calcium Channel Blockers (diltiazem, verapamil), ♡, Grapefruit juice
Follow expected values for women when treating transwomen and vice versa for transmen who have been on hormone therapy for > 6 months
What is transgender patient care?
Found in the GI tract/BBB and has the known function of eliminating xenobiotics (toxins,drugs) and preventing them from entering the bloodstream. AKA anti-absorption pump.
What are P-Glycoproteins/Efflux Pumps?
What is the First Pass Effect?
Rapid (⏩) occurs in heart, kidney, liver, brain
Slow (🐢) occurs in muscle, skin, fat
Poor perfusion caused by disease/condition (heart disease, sepsis, PVD)
What is circulation/blood supply?
An inactive/less active form of a drug that is converted into its active form in the liver; meant to improve absorption/stability/distribution and allow better delivery to target tissues
What are Pro-drugs?