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
Which atypical antipsychotic is least likely to exhibit class effects
Aripiprazole (abilify)
What are the class side effects for atypical antipsychotics?
sedation, orthostasis, anticholinergic effects, EPS, TD, agranulocytosis
Asenapine AKA
(Saphris); Atypical antipsychotic
Brexpiprazole AKA
(Resulti); Atypical antipsychotic
Cariprazine
(Vraylar); atypical antipsychotic
Clozapine AKA
(Clozaril); Atypical Antipsychotic
Iloperidone AKA
(Fanapt); Atypical Antipsychotic
Which atypical antipsychotic is the most likely culprit for agranulocytosis?
Clozapine (Clozaril)
Lurasidone AKA
(Latuda); Atypical Antipsychotic
Olanzapine AKA
Zyprexa; Atypical Antipsychotic
Paliperidone AKA
(Invega); Atypical Antipsychotic
Pimavanserin AKA
(Nuplazid); Atypical Antipsychotic
Quetiapine AKA
(Seroquel); Atypical Antipsychotic
Risperidone AKA
Risperidal; Atypical Antipsychotic
Ziprasidone AKA
Geodon; Atypical Antipsychotic
Lithium (Eskalith) what is the dosing?
900 to 1800 mg/d in divided doses,
When do you get a lithium trough?
serum lithium trough level 12 hours from the previous dose
What is the half life of lithium?
half-life 20 hours,
How often do you check a lithium trough when titrating?
during titration check twice weekly, then every 1 to 2 months when stable.
How long does lithium take to be effective?
Initial anti-mania: 5 to 7 days, full effect 10 to 21 days.
What should you evaluate prior to initiating lithium?
Before initiating, evaluate renal function, electrolytes, thyroid function, EKG, pregnancy test
How does lithium effect pregnancy and breast milk?
contraindicated in the first trimester, associated with Ebstein’s anomaly: right ventricular outflow tract obstruction in the fetus Excreted in breast milk.
What is the therapeutic index for lithium? What about in the elderly?
0.6 mEq/L in elderly, 0.8 to 1.2 mEq/L.
At what age is lithium FDA approved in children?
FDA approved in children >7 years of age.
Lamotrigine (Lamictal) dosing schedule:
25 mg/d × 2 weeks, then 50 mg/d × 2 weeks, then 100 mg/d × 1 week to a maximum daily dose of 400 mg/d.
What is the most serious adverse reaction with Lamotrigine (lamictal)?
Adverse severe reaction: Stevens–Johnson syndrome
What medication can hugely increase the risk of Stevens-Johnson syndrome if taken at the same time as Lamotrigine (lamictal)?
(SJS; risk is increased when used in conjunction with valproic acid).
How does Lamotrigine (Lamictal) effect pregnancy and breast milk?
Can be used in pregnancy with caution if the benefit outweighs risks. Excreted in breast milk; monitor infant for poor sucking, drowsiness, apnea.
How does Lamotrigine (Lamictal) effect pregnancy and breast milk?
Can be used in pregnancy with caution if the benefit outweighs risks. Excreted in breast milk; monitor infant for poor sucking, drowsiness, apnea.
What happens to the half life of Lamotrigine (Lamictal) if taken with valporic acid?
Half-life 30 hours (half-life is doubled when used in conjunction with valproic acid),
How does smoking effect the half life of Lamotrigine (Lamictal)?
smoking induces metabolism and reduces half-life by 50%
Carbamazepine AKA
(Tegretol); Antiepileptic or mood stabilizer
What happens to the half life of Carbamazepine (Tegretol) while on maintenance dosing?
Half-life shortens while on maintenance due to auto-metabolic effect.
Oxcarbazepine AKA
Trileptal; Off label for bipolar
Side effects common to TCAs?
Side effects common to the class include xerostomia, blurry vision, diaphoresis, orthostatic tachycardia, drowsiness, restlessness, and palpitations.
What are the dietary restrictions of MAOIs?
Dietary (tyramine) restrictions: Aged cheese, cured meat, smoked meat, fermented foods, fish sauce, alcohol, and soy products.
Clomipramine AKA
(Anafranil); TCA
Desipramine AKA
(Norpramin); TCA
Amitriptyline AKA
(Elavil); TCA
Doxepin AKA
(Sinequan); TCA
Imipramine AKA
(Tofranil); TCA
Phenelzine AKA
Phenelzine (Nardil); MAOI
Tranylcypromine sulfate AKA
(Parnate); MAOI
Selegiline transdermal AKA
(Emsam); MAOI
Citalopram AKA
(Celexa); SSRI
S-Citalopram AKA
(Lexapro); SSRI
Sertraline AKA
Zoloft; SSRI
Fluoxetine AKA
Prozac; SSRI
Paroxetine AKA
Paxil; SSRI
Vortioxetine AKA
(Brintellix); SSRI
Vilazodone AKA
(Viibryd); SSRI
Nefazodone AKA
(Serozone); SSRI
Trazodone AKA
(Desyrel); SSRI
Levomilnacipran AKA
(Fetzima); SNRI
Venlafaxine AKA
Effexor; SNRI
Desvenlafaxine AKA
(Pristiq); SNRI
Duloxetine AKA
Cymbalta; SNRI
What is the primary receptor target for SSRI?
The primary receptor target is 5-hydroxytryptamine (5-HT)
What are the main side effects for an SSRI?
insomnia (initially and during titration), drowsiness, nausea, dry mouth, diarrhea, restlessness, inhibited arousal (erectile dysfunction), and anorgasmia.
What lab should you monitor for SSRI and SNRI?
Monitor sodium levels in the first 2 weeks. SIADH can occur at any time while on any psychotropic medication
Which two antidepressants are least likely to cause SIADH?
Mirtazapine and buproprion
Besides anxiety and depression what are SNRIs first line for?
neuropathic pain
What are the class side effects for SNRIs?
hypertension, insomnia (initially and during titration), drowsiness, nausea, dry mouth, diarrhea, restlessness, inhibited arousal (erectile dysfunction), anorgasmia, and retrograde ejaculation.
SNRIs and discontinuation
Discontinuation and withdrawal syndromes are usually due to the short half-life of the serotonin component of the medication and occur in up to one-third of patients. Augmenting with a long-acting SSRI can mitigate many of these effects during the discontinuation process
dizziness, fatigue, headache, nausea, agitation, anxiety, insomnia, irritability, electric-like shocks (head zaps), and audio visual hallucinations are symptoms of
Discontinuation symptoms of SNRIs
The concurrent use of benzodiazepines and opioids are an issue because
Concomitant use with opioids can lead to elevated opioid levels through the CYP450 3A4 pathway.
What benzodiazepines are preferred in patients with hepatic diseases or an alcohol use disorder?
Oxazepam, lorazepam, and temazepam
What are the class side effects of benzodiazepines?
psychomotor slowing, temporary cognitive impairment, and rebound anxiety.
When it comes to benzodiazepines: The shorter the half-life,
the more likely the patient will experience withdrawal symptoms.
Which three benzodiazepines have a short half life?
Oxazepam, lorazepam, and temazepam
Alprazolam AKA
Xanax; Benzodiazepine
Chlordiazepoxide AKA
Librium; Benzodiazepine
Clonazepam AKA
Klonipin. Benzodiazepine
Diazepam AKA
Valium; Benzodiazepine
Lorazepam AKA
Ativan; Benzodiazepine
Oxazepam AKA
Serax; Benzodiazepine
What BP med can be used for performance anxiety?
Beta blockers like propranolol (Inderal)
What BP meds can be used for Posttraumatic stress disorder (nightmares), symptomatic support in opioid withdrawal?
Alpha blockers/clonidine, prazosin, doxazosin
dextroamphetamine AKA,
(Adderall); stimulant
methylphenidate AKA
(Ritalin); stimulant
lisdexamfetamine AKA
(Vyvanse), stimulant
Clonidine AKA
Kapvav; alpha agonist
guanfacine AKA
Intuniv; alpha agonist
What are two BP medications that can be used to treat ADHD?
Clonidine and Guanfacine
Neural tube defects, cleft lip, cleft palate, atrial septal defects are birth defects associated with
Antiepileptic drugs (valproic acid, carbamazepine):
Ebstein anomaly (especially in the first trimester) are associated with
Lithium
Floppy baby syndrome, cleft palate are associated with
benzodiazepines
