Exam 2 supplement: medications powerpoint from Summer 2014. Feel free to add/modify to reflect Dr. Thompson's class Flashcards
Definintion: Pharmacology
study of the effects of drugs on the body and the effect of the body on the drugs
Definition: pharmacotherapeutics
sub-category of pharmacology. use of specific drugs to prevent, treat, or diagnose a disease
definition: Pharmacokinetics
subcategory of pharmacotherepeutics (which is a subcategory of pharmacology):
how the body deals with the drug in terms of how it is absorbed, distributed, and eliminated
definition: pharmacodynamics
subcategory of pharmacotherepeutics (which is a subcategory of pharmacology):
Analysis of what the drug does to the body
Definition: Toxicology
study of harmful effects of chemicals
definition: Pharmacy
preparation and dispensing of medications
definition: drug
chemical demonstrated effective for preventing or treating disease
3 types of drug names:
- Chemical
- Trade/brand
- genaric
Definition: Chemical name
non-proprietary, no owner, specific compound’s structure, generally loooooooong.
definition: trade/brand name
owned by a company or companies
definition: genaric name
official or non-proprietary name, often derived from chemical name
Drug approval agency in USA:
FDA (food and drug administration)
4 phases of human testing and attributes of each:
- Phase 1: determine effects & safe dosage; < 100 healthy people
- Phase 2: assess drug’s effectiveness, 200-300 with disorder
- Phase 3: assess safety & effectiveness in larger sample, 1000-3000 with disorder
- Phase 4: monitor any problems that occur after approval
What type of testing is performed before human trials commence?
Preclinical testing, lab tests to determine drug effects and safety
what is the minimum amount of time it can take for a drug to be approved
3 years (but it is usually 7 or more)
How many drug schedules are there?
five (V)
Schedule I drugs: description and 2 examples
highest potential for abuse. not normally used for medical treatment
(marijuana, heroin)
(I thought marijuana was in a lower risk class - look up later)
Schedule II drugs: description and 1 example
approved for specific medical use, high potential for abuse and addiction (morphine)
Schedule III drugs: description and 3 examples
mild-moderate physical dependence, strong psychologic dependence. (opioids, anabolic steroids, amphetamines)
Schedule IV drugs: description and 2 class examples
lower potential for abuse (depressants, stimulants)
Schedule V drugs: description and 2 examples
lowest relative abuse potential (low dose opioids in cough medicine, antidiarrheal preparations)
Five ways to categorize drugs
- Drug action
- chemical
- therapeutic category
- Non-prescription (OTC) - FDA approved
- Prescription - FDA approved
Pharmacokinetics terminology: site of action
where the interaction takes place
Pharmacokinetics terminology: onset of action
where enough drug causes a response
Pharmacokinetics terminology: duration of action
time between onset and termination
Pharmacokinetics terminology: half-life
time required for 50% of drug to be eliminated from body
Pharmacokinetics terminology: clearance rate
measure of efficiency of metabolism or excretion (both are ways of drug removal)
Pharmacokinetics terminology: bioavailability
the amount of drug absorbed and rate of absorption through blood stream
Pharmacokinetics terminology: volume of distribution
target tissue for distribution (for instance, increased body weight might mean a larger dosage is needed to create an effect)
pharmacokinetics is . . .
the study on the impact of the body on drugs
Chemical structure will …
determine biological effect. structures with different chemical make-ups will have different indications, effects, dosage
definition: soluablility
time to dissolve in GI, absorbed in bloodstream, distribution to target tissue, excretion
polarity of drugs is important because
most drugs are both water and fat soluble to some degree (iontophoresis)
Ionization does what for drugs
enhancing the chemical charge, either positive or negative. disolving in solution alters strength of the charge
Administration, absorption, distribution, excretion
part of pharmacokinetics
2 main Routes of administration
- Enteral (oral, sublingual/buccal, rectal)
- Parenteral (intravenous, intramuscular and subcutaneaous, intrathecal [tendon sheath injection], topical, transdermal, inhalation)
First pass effect
occurs when drugs are administered orally and must pass through liver where significant amount of drug may be metabolized prior to reaching site of action
(means oral drug dose might need to be higher than injected drug)
3 types of cell absorption
- Passive diffusion (just need gradient, no ATP, cannot go up gradient)
- facilitated diffusion (need transporter protein, no ATP, cannot go up gradient) - example: glucose entering cell
- Active transport (need transporter protein and ATP, can go up gradient) - example Na+K+ pump
Distribution factors:
- Tissue permeability (think blood-brain barrier) Blood flow to area
- How much of drug is bound to plasma proteins (it will not be available to enter cell if bound in blood)
- binding to subcellular components (how much of drug is stuck inside cells where it cannot leave to be distributed to other locations)
2 ways for excretion
- Renal (most common) - Pee
- Billary (liver bile to small in intestine) - Poop
pharmacodynamics definition
study of impact of drugs on the body
Includes
- molecular mechanisms by which drugs exert therapeutic actions and adverse side effects,
- and Therapeutics, the study of the parameters that determine the most appropriate therapy for a patient)
4 things to consider for Therapeutic parameters
- presence of diseases
- other drugs a person is taking
- dosage regiment of each drug
- impact of potential adverse effects
additive effect
response of 2+ drugs used together: synergistic or antagonistic
Placebo vs placebo effect
placebo: dosage with no active ingredient
placebo effect: response that cannot be attributed to potency of drug
tolerance
diminished response to drug with continued use
3 factors that may cause drug tolerance
- drug metabolizing enzymes - quicker metabolism
- receptor change in number - responsiveness of receptors altered
- affinity to drug: opioids and CNS stimulators (uppers)
agonist vs antagonist drug
agonist drug: causes same effect as body normally produces (but may be larger effect)
antagonist drug: causes the body’s normal reaction to not occur by blocking a receptor
Must have _____ & ______ present for an drug to work.
drug
receptors
4 dose types
- single dose: dose required for a certain response
- multiple dose: greater blood concentration increase than single dose, levels off when bio-availability = clearance rate
- Maintenance dose: regular interval in repetitive basis
- Loading dose: starter dose to get a higher blood level quicker and then return to maintenance dose
5 therapeutic considerations
- patient compliance
- dose
- therapeutic monitoring
- age (children are smaller, elderly have decreased organ functioning)
- liver/kidney function testing
2 types of drug interactions
- synergistic (additive/agonistic effect): increases effect of drug
- Detrimental/antagonistic effect: decreases effect of drug (think antibiotics with birth control)
ADR
Adverse Drug Reactions
7 Adverse drug reactions (ADR)
- side effects (non-therapeutic effects)
- Allergic reaction
- Organ cytotoxic effects
- idiosyncratic reaction (strange reaction)
- Drug-drug interactions
- Drug-food interaction
- Drug-herbal interaction
What is an example of a medication highly influenced by food?
Coumadin (Warfarin)
Muscle relaxants are for what (general category & 2 subcategories)?
Hyperexcitability:
- muscle spasm,
- spasticity
Do muscle relaxants prevent muscle contraction?
no. They just normalize muscle excitability to decrease pain and increase function
What is a muscle spasm?
increased tension most seen in skeletal muscle after MSK injuries and inflammation
what is the most common route of administration for muscle relaxants?
oral
Diazepam (Valium)
4 things
- Oldest medication to treat muscle spasms.
- also treats spasticity.
- can cause physical dependance
- also used for anxiety
Diazapam negative effects (4)
- sedation
- general reduction in psychomotor ability
- tolerance –> dependence
- withdrawal symptoms if stopped suddenly (seizures, anxiety, agitation, tachycardia, DEATH)
Polysynaptic inhibitors are used for what?
muscle relaxants used for short term relief of muscle spasms associated with acute, painful MSK
Adverse effects of polysynaptic inhibitors (a muscle relaxant class)? (4 main categories)
- Drowsiness
- Dizziness
- Nausea, light-headedness, vertigo, ataxia
- Long term use may cause tolerance and physical dependence.
Polysynaptic Inhibitors often have what in their brand name
flex or x
7 Poly-synaptic inhibitors - ways to remember and beginning of generic name
- 4 C’s, 2 M’s, 1 O.
- 4 Cs: Girl’s names + monster: Cari, 2 Chlo (e), Cyclo (pse).
- 2 Ms: Meta and Meth. Meta-ex-alone (alone because of ex) & Meth-o-carb (meth and carbs are bad to some people)
- 1 0: Orphen (all alone as an orphan)
Which polysynaptic inhibitors does Dr. Henderson use the most?
Flexeril & Robaxin
Cyclo (pse) & Meth-o-carb
Three things about Opioid Analgesics
- naturally occurring, semisynthetic & Synthetic relieve moderate to severe pain
- bind to specific neuronal receptors in CNS
- controlled substances (usually schedule II or III)
4 Classifications of opioids
- Strong agonists
- mild-moderate agonists
- mixed agonist-antagonist
- antagonists
Opioids: Strong Agnonist,
purpose and
characteristics of generic name.
2 common brand names
For: Severe Pain
Name: Morph (morphine, -morphone)
Brand: Demoral, Hydrostat
Opioids: mild-moderate Agnonist,
purpose and
characteristics of generic name.
1 common brand name
Purpose: moderate intensity pain
Name: Code (codine, codone)
brand: OxyContin
Opioids: mixed Agnonist-antagonist,
attributes (why use/different) and
characteristics of generic name.
Safer, not common, not as strong as others.
Name: lots of Bu (But-, Bup-, Nal-Bup)
Opioids: antagonists,
purpose and
characteristics of generic name.
Treat Overdose
Name: Nal- (nalmefene, naloxone, naltrexone)
Adverse effects of opioids (7 descriptions):
- Strong physical dependance risk
- Potential for abuse
- Sedation,
- respiratory distress
- Constipation
- psychotic effects
- Cardiovascular effects (our friend orthostatic hypotension)
Opioids: clinical applications (6)
- Effective for treating moderate-severe pain that is constant in duration.
- Not as effective for treating sharp, intermittent pain
- Work on altering perception of pain rather than eliminating pain sensation
- Parenteral routes may be more beneficial for chronic or severe pain
- Influenced by dosing schedules
- In-dwelling catheters can be implanted
NSAIDs: purpose and not the same as ______
Used to decrease inflammation, relive pain, reduce fever, decrease blood clotting
Not the same as glucocorticoides (which are also used to treat inflammation). Glucocorticoids are steroids.
Two types of NSAIDs based on mechanism of action:
Non-selective (block COX-1 and COX-2)
Selective (block COX-2 only)
COX-1 vs COX-2
both work on prostaglandins.
COX-1 related to stomach lining protection, renal function, and platelets.
COX-2 only mediate pain and inflammatory response
What are two side effects of non-selective NSAIDs?
Primary: GI damage
Renal Damage
What is the only selective COX-2 inhibitor on the market now (and do you need a prescription)?
Celebrex
Prescription needed
Is Tylenol (acetometaphin) an NSAID, and where is it metabolized?
No
In the liver
Therapists should watch out for multipharmacy and interaction concerns missed by other caregivers. We spend the most time with patient.
cheers (you get this one free)
