Pharmacology Exam 2 Flashcards
Liraglutide: Indication and distribution
Primarily - DM2
Also used as an anorexiant
highly bound to protein
Anorexiant MOA
Sympathomimetic amines → stimulate the satiety centers in the hypothalamus and limbic regions
- noradrenergic, dopaminergic, or serotonergic pathways
Anorexiants: Contraindications
- General
- Liraglutide
- Lorcaserin
DM - can cause hypoglycemia
Liraglutide - Pregnancy: due to wt loss
Lorcaserin -
- Pregnancy due to category X
- other drugs that increase serotonin
- <18 yo
Anorexiants: ADRs
- General
Hypoglycemia - decreaed intake
CNS overstimulation and agitation, confusion, insomnia, dizziness, hypertension, headache, palpitations, arrhythmias, dry mouth, mydriasis, dysuria, constipation, vomiting, diarrhea, and impotence
ADRs
Liraglutide
N/V/D
- Hypoglycemia
- Suicidal Ideation
- Slowed gastric emptying – may alter other drug’s absorption
ADRs
Lorcaserin
Suicidal ideation
stimulate ADRs
euphoria/hallucinations
priapism/prolactin
CBC changes
hypoglycemia
Anticonvulsants (AEDs): Precautions
- Increased risk for suicidal thoughts
- Monitor seizure activity
- associated with fetal defects
- suicidal ideation
- lactation
Anticonvulsants: Topiramate MOA
Inhibition of carbonic anhydrase → may lead to increased renal bicarb LOSS → metabolic acidosis
Inhibition of carbonic anhydrase can also lead to increased ammonia levels
Phenytoin (Hydantoin)
- MOA
- Blackbox Warning
- Common Hypersensitivity
- Newborn who have been exposed
- blocks Na+ - decreased potential
- IV < 50mg/min in adults and 1-3mg/kg in peds
- Phenytoin-induced hepatitis is a common hypersensitivity
- Newborns need Vit K
Phenytoin (Hydantoin): Common Drug Interaction
IBUPROFEN – increases dilantin lvls
Phenytoin monitoring
LFTs,CBC with diff, UA
Drug levels
Assess for phenytoin hypersensitivity syndrome → fever, rash, lymphadenopathy → typically weeks 3-8
Phenytoin (Hydantoin): Education
Good oral hygiene – tenderness
Urine may look pink, red, or reddish brown
DM - inhibits glucose stimulated insulin release - hyperglycemia
Phenytoin indication
Seizures, status epilepticus
Carbamazepine indications
epilepsy, bipolar disorder, trigeminal neuralgia, aggressive behavior
Carbamazepine: MOA - including additional
Decreases the amount of Na+ going into cortical neurons → decreases action potential → decreased seizure activity from interrupting the abnormal neuronal discharge
Alos: anticholinergic, antidiuretic, antidysrhythmic, and antidepressant activity
Carbamazepine: Metabolism
Self-induced – therapeutic ranges may fall
Carbamazepine: Precautions
-include Black Box Warning
Intraoccular pressure – due to anticholinergic affects
grapefruit juice increases drug levels
Decrease TSH
Black Box Warning: SJS - Screen asian patients for HLA-B*1202 gene
Black Box Warning: May cause blood dyskrasias – leukopenia, thrombocytopenia, agranulocytosis, and aplastic anemia
Carbamazepine: screening
SJS and toxic epidermal necrolysis → particularly among asians
Screen asian patients for HLA-B*1202 gene
Carbamazepine: Contraindications
pregnancy: CATEGORY D
Hypersensitivity to Carbamazpines or TCAs,
hx of bone marrow suppression,
concurrent administration with MAOs
Carbamazepine can decrease levels of the following drugs:
Beta blockers, warfarin
Carbamazepine: Monitor
Baseline CBC, chemistry, LFT, Renal function, CMP, TSH/ T4 → then frequently → then every 3-4 mo if nrml
Carbamazepine → drug levels
Lamotrigine: Indications
seizure, bipolar disorder, mood
Lamotrigine: MOA
decraese sodium channels and inhibits the presynaptic release of glutamate and aspartate in the neuron
Carbamazepine: Side Effects
N/V, dizzy, drowsy, DRY MOUTH, feels like swollen tongue
Lamotrigine: Precautions
- includingn Black Box Warning
Multi-organ failure - DIC → begin as fever or lymphadenopathy
BLACK BOX WARNING
Life-threatening rashes: SJS, TEN, and rash-related death → more likely in peds
Coadmininstration with valproate may increase risk of rash
Lamotrigine: Drug interactions
Many → due to CYP450
Estrogen → decrease Lamictal
Rifampin → decreases Lamictal
Valproate → increased chance of life threatening skin rash
Succinimides [ethosuximide (Zarontin)]:
- Indication
- Pregnancy
Indication: Seizures
Appears safe in pregnancy
Birth control → succinomides may decrease effectiveness of birthcontrol
Zosinamide:
- Indication
- Drug Interactions
Seizures
Used with other carbonic anhydrase inhibitors (topiramate, acetazolamide, dichlorphenamide) → may increase risk of metabolic acidosis
Zosinamide: Distribution
extensively bound to erythrocytes
- 40% bound to proteins
Topiramate: Indication
Gabapentin: Indication
T - Seizures, migraine prophylaxis
G- Seizures, migraine prophylaxis
Gabapentin and Topiramate: Metabolism
G: Not metabolized – excreted unchanged in kidney
T: Isn’t metabolized a lot
Gabapentin : Side Effects
aggression/hostility
suicidal ideation (all AEDs)
Topiramate: Adverse effects
vision problems
oligohydramnios and hyperthermia
inhibition of carbonic anhydrase → may lead to increased renal bicarb LOSS → metabolic acidosis
Inhibition of carbonic anhydrase can also lead to increased ammonia levels
dizziness, drowsiness, fatigue
impaired concentration/memory
nervousness, speech problems
nausea, weight loss
ataxia
photosensitivity
behavioral problems, mood problems
anorexia
Topiramate: Monitoring
electrolytes (esp bicarbonate)
intraocular pressure
body temp/sweating
Perampanel:
- Indication
- MOA
- SE
Indication: Seizurs
MOA: AMPA antagonist
SE: Hosility, aggression, agitation, anger, homicidal
Dizziness and gait disturbances
Levetiracetam:
- Indication
- Metabolism
- SE
Indication: Seizures
Metabolism:
Less than 10% protein bound
Doesn’t use CYP450
SE: Alopecia –> reversible
What are the cardiac effects of TCA antidepressants?
- tachycardia d2 inhibition of norepinephrine uptake and anticholinergic effects when TCAs block acetylcholine
- slowing of depolarization contributes to a prolonged QRS and subsequent QT interval.
Which malignant neoplasm is carbidopa-levodopa known to activate?
Melanoma
How do you dc lorazepam (Ativan)?
- Decrease the dose by 0.5 mg per week, then by 0.25 mg for the last few weeks.
- Switching to a shorter-acting benzodiazepine, not a long-acting agent.
Benzodiazepines increase the levels of what two drugs?
TCAs and digitalis
TCA: adverse reactions
- Histamine: drowsiness and weight gain
- Tachycardia due to decreased norepinephrine reuptake and anticholinergic
- Prolongation of QRS and PR/QT intervals
- Anticholinergic adverse effects are common and can include dry mouth, constipation, urinary hesitancy or retention, blurred vision, sedation, orthostatic hypotension, weight gain, nausea and vomiting, gynecomastia, and changes in libido
- older adults: anticholinergic and norepinephrine effects→ confusion, orthostatic hypotension, and falls
Why shouldn’t you use MAOIs when you are on TCAs?
can cause hyperpyrexia
TCA contraindications
- Cardiac disorders: alpha-adrenergic blocking effect and quinidine-like effect on the myocardium
- MAOIs → hyperpyrexia
- High risk of suicide
TCA precautions
- Overdose can be fatal - makes them less safe to use in patients who are a high risk for suicide
- Glaucoma, prostatic hypertrophy, & urinary incontinence: d2 anticholinergic effects
- Older adults: anticholinergic and norepinephrine effects→ confusion, orthostatic hypotension, and falls
- Be alert for an energizing effect that precedes depressive symptom remission because this may contribute to sufficient neurocognitive activation to follow through with a suicidal plan