Exam 1 - Math / Interactions / Absorption Flashcards
1 pound
16 ounces
1 ton
2000 pounds
1 cup
8 oz
1 pint
2 cups
1 quart
2 pints
1 gallon
4 quarts
3 base units of metric system
- length (m)
- volume (L)
- weight (g)
Order of metric bases
Kilo Hecto Deka (Unit) Deci Centi Milli
Abbreviation for micron
mc
1 kg
2.2 pounds
1 pound
454 grams
1 inch
2.54 cm
1 teaspoon
5 mls
1 tablespoon
15 mls
1 Liter
1.06 quarts
Weight volume solution
Solid is solute
Volume volume solution
Liquid is solute
ml or cc on chart?
- mL
gtt
Drops
Types of syringe tips
- lure lock
- slip
- eccentric
- catheter
Macrodrip
- fast infusion
- fluid resuscitation
- drug bolus
- potential for overdose
- bad for titration
Microdrip
- good for titration
- avoids overdose
- no resuscitation
- bad for large bolus
Isotonic solution
- 0.9 NaCl
- 5% Dex
Naming of drugs
- Brand name = Advil
- Generic name = Ibuprofen
- Chemical name = blah blah blah
Indications / Usage
- FDA-approved
- reasons why you would take drug
Contradictions
- warnings
- who should not take drug
- when you shouldn’t take drug
Drug interactions happen when:
- combo therapy is preferable/necessary to produce effect
- single pathology may have multiple symptoms
- may suffer from more than one pathology
- modification of drug effect when given with another drug
Beneficial drug interaction
- drug combo therapy
Harmful drug interaction
- adverse side effects
Addictive interactions
- Adds two drug effects for overall greater effect
- doubling up
Synergistic drug interactions
- bad if used together
- too much effect (overkill)
Potentiation drug interactions
- one drug increases the response of another drug, which normally has lesser effect
Adverse drug reactions (ADR)
- unintended side effects
- 5% of hospitalization
- tremors / bronchospasm / headache / vomiting / etc
- Not all ADRs are allergies
Drug allergy
- immune mediated
- induce hypersensitivity rxn
- mild hives to anaphylactic shock
- one example of an ADR
Pharmacokinetics
- what body does to a drug
- Absorption (input)
- move from admin site to plasma
- rate limiting is how fast it is dissolved
- Small / non polar / lipophillic will go through
- Distribution
- dissemination of drug through body
- bloodstream is major vehicle
- influenced by flow / solubility / protein binding
- Metabolism
- transformation into secondary components (metabolites)
- preparing drug for elimination…more water soluble
- performed by liver… cytochrome P-450 enzyme systems
- Elimination (output)
- removal via urine, bile, feces
- also via pulmonary, skin, hair, saliva, and expiration
Pharmacodynamics
- what the drug does to the body
Routes of administration
- determined by property of drug
- solubility
- ionization
- how fast we want it to act
- need for long term treatment
- if need to restrict to local site
Enteral
- through digestive tract
- usually through mouth
- most common / safest / convenient / economical
Parenteral
- through outside of digestive tract directly into circulation
- IV / IM / SC
- Good:
- drugs poorly absorbed via GI
- patients who can’t take oral drugs
- need rapid onset
- highest bioavailability
- most control over dosage
- Bad:
- irreversible
- cause pain and fear
- local tissue damage
- infections
Sublingual
- under tongue
- bypass GI
- rapid absorption
Buccal
- Between gums and cheek
- directly into circulation
- bypass GI
- rapid absorption
Oral administration
- easily self administered
- antidote for overdose
- low stomach pH inactivated some drugs
- can use enteric coating to get to small intestine
- enteric coating good for acid unstable drugs
- most complicated absorption
Extended release prep
- special coatings or ingredients that control release
- slow absorption
- prolonged duration of action
- less frequent dose (improved compliance)
- useful for short half lives
IV
- drug into vein
- most common parenteral route
- rapid effect / max control
Bad:- infection
- hemolysis
- no drug recall
- ADRs
IM
- directly into muscle
- aqueous solutions absorbed fast
- specialized depot preps
SC
- into subcutaneous tissue of skin
- via diffusion
- slower drug onset vs IV
- constant, slow, sustained effects
- insulin
Oral / Nasal
- airways and lungs
- rapid delivery
- patients with respiratory disorders
- direct delivery to site of action
Intrathecal / Intraventricular
- into cerebrospinal fluid
- rapid delivery
- good if need to bypass blood-brain barrier
- epidural / antibiotics for meningitis
Topical
- onto skin
- good for local effect
- acne
Transdermal
- via the skin
- gets into systemic circulation
- control rate of absorption
- sustained delivery
- patches
Rectal
- via rectum
- avoid stomach acid
- good to avoid vomiting
- Bad:
- erratic and variable absorption
- irritate rectum
- not well accepted route
Rate of absorption depends on:
- environment
- chemical characteristics of drug
- route of admin
Oral cavity
- slightly acidic
- thin epithelium / high vascularity
- bypass hepatic system (no 1st pass)
Stomach
- very acidic
- folds increase SA
- no absorption
- just digestion
Small Intestine
- site of absorption
- deep folds with villi and microvilli
Large intestine
- little absorption (just water and Na)
- bypass hepatic system
Absorption mechanisms from GI
- Passive (aqueous or lipid)
- Facilitated
- Active
- Endo/Exocytosis
Passive diffusion
- most common mechanism for drugs
- [ ] gradient is driving force
- not saturable
- low specificity
- through aqueous channel pore or lipid membrane
Fick’s law
- applies to aqueous and lipid
- Net diffusion = (area)([ ] gradient) / thickness of membrane
Facilitated diffusion
- via transmembrane carrier proteins
- conformational change allows passage
- high [ ] to low [ ]
- no energy
- saturable
- inhibited by competitors
Active transport
- drugs that resemble natural metabolites
- energy dependent
- against gradient
- saturable
- selective
- competitively inhibited
Endo and Exocytosis
- for large molecules across membrane
- in or out
Factors that influence absorption
- pH
- Blood flow (direct)
- intestine gets more flow so intestine is favored
- in shock… low skin flow makes SC absorption poor
- Surface area (direct)
- intestines have 1000x greater than stomach
- Contact time
- Stomach…slow emptying = decrease absorption
- intestine… slow transit time = better absorption
- P-glycoproteins
- transmembrane transport protein that pumps out drugs
- reduces drug absorption
- liver / kidneys / placenta / intestines / brain
Acidic drugs
HA H+ + A-
- release a proton
- HA is drug
- acidic environment shifts rxn left
- acidic drugs more soluble in acidic pH and visa versa
Basic drugs
BH+ B + H+
- accept protons
- B is drug
- basic environment shifts rxn right
Low pKa
- more acidic drug is
High pKa
- more basic drug is
pH < pKa
- protonated form dominates
- HA and BH+
pH > pKa
- deprotonated form dominates
- A- and B
Clinical application of pH of drugs
- can trap in urine by ionizing them
- acidic drugs excreted faster in basic urine
- basic drugs excreted faster in acidic urine
- can also trap drugs in:
- stomach
- small intestine
- breast milk
- aqueous humor
- vaginal/prostatic secretions
Bioavailability
- fraction of drug unchanged following administration
- important foe calculating drug dosages for non-IV
- determined by:
- compare plasma levels of drug after IV admin
- compare plasma levels of drug after non-IV admin
- Area under curve is extent of absorption
- %BioComp. = AUC oral / AUC IV
Factors that influence bioavailability
- 1st pass hepatic metabolism
- decreases absorption if goes through 1st pass
- solubility of drug
- hydrophilic poorly absorbed
- extremely lipophilic also poor
- ideal is weak acid / weak base
- chemical instability of drug
- pH of stomach can lead to this
- Degradative enzymes in GI tract too (like on insulin)
- nature of drug formulation
- particle size
- salt form
- enteric coatings
- binders and dispersing agents
Drug pathway
- 1st dissolved
- 2nd absorbed
Bioequivalence
- comparable:
- Bioavailability
- Time to peak [ ]
Pharmaceutical equivalence
- Bioequivalent but also:
- same amount of active drug
- same dose
- same admin route
Therapeutic equivalence
- Bioequivalent
- Pharmaceutically equivalent but also:
- Comparable:
- clinical effect
- safety profile
- These are generic drugs