PMHNP Certificate Study Guide Pharmacology Flashcards
The movement of the drug into the bloodstream.
Absorption
The movement of the drug through the bloodstream and to target receptors.
Distribution
The transformation or breakdown of the drug in preparation for elimination from the body
Metabolism
The precirculation process (uptake and conversion) by which the substrates (changed drug) are significantly reduced by the cytochrome P450 (CYP450) enzyme in the liver after enteric absorption.
First Pass Effect
The process by which substances (drugs, substrates, toxins) leave the body (feces, urine, skin).
Excretion
The time needed to clear 50% of the drug from the plasma
Half Life
How many half lives does it take to clear a drug from circulation completely?
5
How many half lives does it take to create a “steady state” for medications?
5
Speeds up the metabolic rate, decreasing serum level of the drug
Inducing
Slows down the metabolic rate, increasing the serum level of the drug
Inhibiting
A special medication consideration for young children especially during periods of rapid growth and development
metabolize (CYP450, 2C9, 2C19, 2D6, and 3A4) more rapidly, thereby causing lower drug concentrations (available free drug) in the systemic circulation (subtherapeutic dose).
A special medication consideration for the elderly?
Elderly patients metabolize (CYP450, 1A2) more slowly, thereby causing higher concentrations (available free drug) in the systemic circulation (increased risk of toxicity).
These type of metabolizers have two defective genes and complete absence of the enzyme, for example, CYP2D6.
Poor metabolizers
These type of metabolizers have variant genes that are less effective in producing the catalyst.
Slow metabolizers
These type of metabolizers have two functional “wild-type” genes. This is normal drug metabolism.
Extensive
These type of metabolizers have more than two copies of the gene and excessive production of the enzyme.
Ultra Rapid
Liver disease affecting enzyme activity (first-pass effect) can have an inhibitory effect which in turn
increasing the risk of drug toxicity
Renal insufficiency (or acute kidney injuries) can also lead to this problem due to reduced glomerular filtration rate (GFR).
increased serum concentrations
Low muscle mass, reduced protein, and increased fat stores can lead to what problem with medications?
increased drug concentrations and risk of toxicity
Intracellular volume can effect drug metabolism. How does it effect pregnant women and the elderly?
Reduced in the elderly requiring a decreased dose, but increased in pregnancy which can necessitate an increased dose.
the study of drug action on the body, specifically the relationship between drug concentration and effect (dose and response).
Pharmacodynamics
The process of becoming desensitized and therefore less responsive to a particular dose of medication over time, necessitating increases; may eventually lead to “poop-out” effect.
Tolerance
Rapidly diminishing responsiveness to increasing doses of the medication, aka “poop-out” effect.
Tachyphylaxis
The activation of a receptor by a chemical to produce a biological response.
Agonist
A chemical that binds to a receptor but does not fully activate the receptor and the biological response may be muted
Partial agonist
An agent that binds to the same receptor as an agonist, but induces an opposite biological response.
Inverse Agonist
The blocking of the receptor to inhibit the biological response. This also blocks endogenous agonists from binding.
Antagonist
The substrate may block the various ion channels (potassium, sodium, calcium, chloride) rather than receptor sites and exert either an inhibitory or excitatory effect across the cell membrane.
Ion Channel Blockers
Patients should be informed that standard practice typically recommends lifelong treatment for
bipolar, schizophrenia, refractory depression, and anxiety.
In general what should antipsychotics be monitored for…
significant decrease in the absolute neutrophil count (agranulocytosis), can prolong the QTc interval, and can precipitate the syndrome of inappropriate antidiuretic hormone (SIADH).
This medication requires requires explicit registration in the Risk Evaluation and Mitigation Strategies (REMS) database.
Clonazapine
For SSRIs, SNRIs, and MAOIs you should intermittently monitor…
sodium
Tobacco products are known
CYP450 inducers.
The shorter the half-life, the more difficult
it is to wean
Medications with longer half-lives often have less
intense withdrawal symptoms
First generation antipsychotics are what kind of neurotransmitter disrupter?
Dopamine Antagonists
Which receptor do first generation antipsychotics block?
D2
Chlorpromazine AKA
Thorazine; 1st gen antipsychotic
Fluphenazine AKA
Prolixin; 1st gen antipsychotic
Haloperidol AKA
Haldol; 1st gen antipsychotic
Perphenazine AKA
Trilafon; 1st gen antipsychotic
Thioridazine AKA
Mallaril; 1st gen antipsychotic
What are the general side effects of first generation antipsychotics?
sedation, orthostasis, anticholinergic effects, QTc prolongation, EPS, TD, agranulocytosis
What mood stabilizer do you avoid if you have renal disease?
Lithium
What mood stabilizer do you avoid if you have hepatic disease or female of child-bearing age
Valproate
Which two atypical antipsychotics do you avoid if you have a history of extrapyramidal side effects?
aripiprazole and risperidone
Which three atypical antipsychotics do you avoid if you are obese?
olanzapine, quetiapine, and risperidone
Valproic acid AKA
(Depakene); antileptic also used for mood stabilizer
What is the dosing for Valporic Acid (Depakene)?
60 mg/kg/d in divided doses
When do you get a trough for Valporic Acid (Depakene)?
serum trough level 12 hours from the previous dose,
What is the half life of Valporic Acid (Depakene)?
half-life 13 hours
During titration of Valporic Acid (Depakene) how often do you check a trough?
during titration check twice weekly, then monthly.
What is the therapeutic range for Valporic Acid (Depakene)?
Therapeutic range: 50 to 125 mcg/mL (evaluate for signs of toxicity and improvement of manic symptoms).
If a patient develops an abnormal mental status on Valporic Acid (Depakene) what do you check for?
If patient develops altered mental status, evaluate for hyperammonemia.
If a patient is outside the therapeutic range for Depakene but remains asymptomatic what should you do?
Do not treat if asymptomatic
Valporic Acid (Depakene) effect on pregnant women, breastfeeding, and children
FDA approved in children for seizure disorders, teratogenic, excreted in breast milk
What kind of monitoring do you do for someone on Valporic Acid (Depakote) besides a trough?
Mental status changes, complete blood count (thrombocytopenia), and liver function (transaminitis)
Aripiprazole AKA
(Abilify); atypical antipsychotic