G and G chapter ends Flashcards
Alosetron indication other than nausea
IBS-D
Zofran MOA
5HT-3 antagonist
Lorcaserin MOA
5HT-2c agonist
Lorcaserin indication
Weight loss
Scary side effect of lorcaserin at supraclinical doses
Hallucinations
Triptans MOA
5HT-1b and d agonist
Triptans contraindicated in what patients?
Ischemic heart disease and coronary artery vasospasm
Which Triptans have drug interactions with cyp 3a4 inhibitors?
Eletriptan and naratriptan
Can MAOI’s affect Triptans?
Yes, avoid
4 Most common side effects with triptans
Dizziness, sleepiness, neck and chest pain
Triptans safe in pregnancy?
No
Triptans safe in breastfeeding?
No
Can triptans be used concomitantly with SSRI’s/SNRI’s?
Not recommended due to serotonin syndrome
Methylergonovine MOA
Broad 5-HT action
Methylergonovine indication
Prevent post-partum hemorrhage
High dose Methylergonovine can cause what unpleasant side effect?
Sustained uterine contracture
Buspar MOA
Partial agonist 5-HT1a and D2
Flibanserin MOA
5-HT1a agonist and 5-HT2 antagonist
Flibanserin indication
Hypoactive sexual desire in premenopausal women
Cabergoline MOA and indication
Dopamine agonist, Parkinson’s and hyperprolactinemia
Bromocriptine MOA and indication
Dopamine agonist, Parkinson’s and hyperprolactinemia
Rotigotine moa
Dopamine agonist
Main reason cabergoline and bromocriptine are avoided
Cardiac issues (valvulopathies)
Side effect of dopamine agonists (mirapex, requip…) early in parkinson’s
Impulse control
What benefit from use of clozapine in terms of side effects?
Less EPS
Why vraylar or rexulti for schizophrenia?
Improved side effect profile
Can adderall be used in patients that also have bipolar?
Not likely, can worsen psychosis
What side effects does vilazodone lack?
Sexual and weight gain
Milnacipran moa
SNRI
Duloxetine and milnacipran contraindicated in what?
Uncontrolled narrow angle glaucoma
Doxepin drug class
TCA
Desipramine drug class
TCA
How long to wait after taking MAOI to take TCA?
14 days
Blood pressure side effect of TCA’s
Orthostatic hypotension
3 indications of atypical antipsychotics
Depression, schizophrenia, and bipolar
Isocarboxazid drug class
MAOI
Tranylcypromine drug class
MAOI
MAOI’s can cause what side effect if tyramine containing foods/drinks eaten?
Hypertensive crisis
Trazodone and remeron moa
5-HT2 antagonist
Trazodone and remeron dose for successful sleep
Low dose
Why avoid nefazodone?
Risk of liver failure
Chlorpromazine drug class
1st gen antipsychotic
Chlorpromazine hits what 4 receptor types? What are side effects from each receptor type?
D2, muscarinic, histamine, and A1. EPS, anticholinergic, sedation, and hypotension
How can chlorpromazine effect the skin?
Photosensitivity
Haldol has higher rates of which 3 side effects?
EPS, akathisia, and hyperprolactinemia
Hyperprolactinemia manifestations
Infertility, decrease BMD in women, and erectile dysfunction and gynecomastia in men
Haldol causes less of which 4 side effects?
Anticholinergic, sedation, weight gain, hypotension
2 mg Haldol is equivalent to ___ mg chlorpromazine
100
Thiothixene drug class
1st gen antipsychotic
Perphenazine drug class
1st gen antipsychotic
Loxapine drug class
1st gen antipsychotic
Which 2 1st gen antipsychotics have the least EPS and akathisia?
Perphenazine and loxapine
Asenapine
Saphris
Can saphris ODT be swallowed?
No, will be dismantled by liver
Saphris counseling point when administering
Avoid water for 10 minutes after taking
How much effect does asenapine have on weight gain?
Minimal
What 2 GI and oral side effects does clozapine have?
Constipation and drooling
Iloperidone drug class
Atypical antipsychotic
4 common side effects of atypical antipsychotics
Anticholinergic, sedation, weight gain, and hypotension
Counseling point on Latuda administration
Take with 350 cal food
Olanzapine has dose dependent ___ effects
Anticholinergic
Invega has high rates of which side effect?
Hyperprolactinemia
Which 3 side effects are most common with Quetiapine?
Weight gain, sedation, and hypotension
Which 2 atypical antipsychotics have high rates of hyperprolactinemia?
Risperidone and paliperidone
Ziprasidone administration counseling point
Take with 500 cal food
Ziprasidone has improved tolerability if you need to start at high starting dose of ___ mg per day how?
With food
Abilify has low risk of which 2 side effects?
Weight gain and hyperprolactinemia (actually lowers prolactin)
Nuplazid
Pimavanserin
Nuplazid moa and indication
Parkinson’s disease psychosis. 5-HT2a inverse agonist without D2 affect
With Cyp3a4 inhibitors, do what to Nuplazid dose?
Decrease by 50% to avoid overdose
Clinical effects of Nuplazid take how long to be seen?
4-6 weeks
Monitor what 3 labs with lithium?
TSH, lithium level, and renal function
Therapeutic serum level for lithium in acute mania
1-1.5 meq/ml
Maintenance therapeutic serum level for lithium
0.6-1 meq/ml
Lithium may cause what 2 physical side effects?
Tremor, hair loss
What 3 labs are monitored with divalproex?
Divalproex level, CBC, and liver function
Avoid rapid dose escalation for carbamazepine to avoid ___ and ___
Sedation and ataxia
Why slow dose increase for lamotrigine?
To avoid SJS
What to do if patient on lamotrigine and divalproex?
Reduce lamotrigine dose by 50%
How does phenytoin affect cyp3a4?
Induction
2 Common phenytoin side effects
Gingival hyperplasia and facial coarsening
5 common side effects of carbamazepine
Drowsiness, vertigo, ataxia, blurred vision, increased seizure frequency
Which anti seizure meds reduce half life of lamotrigine?
Phenytoin, carbamazepine, and phenobarbital
Why did they make oxcarbazepine?
Less side effects and cyp induction
Lacosamide moa and indication
Sodium channel modulator, epilepsy
Ethosuximide moa and indication
Calcium channel blocker, epilepsy
6 common side effects of ethosuximide
GI, sleepiness, lethargy, dizziness, headache, (rash) hypersensitivity
Zonisamide 4 common side effects
Sleepy, ataxia, anorexia, fatigue
Zonisamide moa
Calcium channel blocker
Abrupt withdrawal of benzos can facilitate what symptom?
Seizures
Infinite levels can be increased in cyp___ poor metabolizers
2c19
Phenobarbital 2 common side effects in children:
Irritability and hyperactivity
Phenobarbital 2 common side effects in elderly
Agitation and confusion
Primidone moa
GABA enhancer
Primidone is a cyp 3a4 ___
Inducer
Fycompa
Perampanel
Perampanel
Fycompa
Fycompa 6 common side effects
Fatal, eYesight, Confusion, Offensive, iMbalance,P, Anxiety
Anxiety, confusion, imbalance, vision problems, aggression, suicidal thoughts
Fycompa moa
Glutamate receptor antagonist
Keppra 5 common side effects
slacKness, Emotionality, Poor focus, Restful, Ataxia.
Sleepy, weakness, ataxia, dizziness, mood changes
3 common topiramate side effects
Sleepy, fatigue, brain fog
Why did they make rytary?
Mixed immediate and extended release sinemet to prevent wearing off effect
3 Most common side effects of dopamine agonists (requip, mirapex…)
Sleepy, impulse control disorder, psychosis
Apomorphine drug class and indication
Dopamine agonist, Parkinson’s rescue for off episodes
Apomorphine must be used concurrently with what?
Nausea meds
Apomorphine is contraindicated with which drug class?
Zofran (5-ht3 antagonists)
Neupro
Rotigotine
Rotigotine
Neupro
Why are COMT inhibitors used in Parkinson’s?
To reduce peripheral metabolism of levodopa, increasing efficacy and half life
Entacapone drug class
COMT inhibitor
Why would rasagiline or selegeline be used in Parkinson’s?
As MAOI’s, they increase dopamine levels.
Max efficacious dose of selegiline in Parkinson’s: ___mg
40 mg
Amantadine effective at treating levodopa induced:
Dyskinesias
Rivastigmine moa and indication
Acetylcholinesterase inhibitor, dementia (Parkinson’s and alzheimer’s)
What is main dose limiting side effect of aricept?
GI symptoms (NVD)
Exelon patches have less of what side effect?
GI (NVD)
Memantine moa
NMDA antagonist (reduces glutamate excitation which leads to damage)
Tetrabenazine moa and indication
Depletes pre-synaptic catecholamines, treats tics (Huntington’s chorea)
2 main side effects tetrabenazine
Hypotension and suicidal depression
Baclofen moa
GABA receptor agonist
Which 4 benzos have the indication for alcohol withdrawal?
Chlordiazepoxide, valium, Ativan, and oxazepam
Flumenazil indication
Benzo ovedose
Belsomra moa
Orexin antagonist
Ballpark phenobarbital half life
Long
Levorphanol 2 unique Side effects
Delirium and hallucinations
As an opioid, why is loperamide sold OTC?
Poor BBB penetration, great for diarrhea
Why is diphenoxylate formulated with atropine?
Atropine side effects of weakness and nausea discourage abuse of the opioid component
What syndrome does delsym increase risk for?
Serotonin syndrome
Naltrexone boxed warning:
Contraindicated in liver failure and hepatitis due to dose dependent liver injury
Precedex should be used only up to ___ duration sedation
24 hours
Dexmedetomidine moa
A2 agonist
How long to apply lidocaine/prilocaine for onset of action?
30 minutes
Do not use Emla cream where topically?
Mucous membranes and open wound
Acamprosate indication
Alcoholism
Diuretic used for altitude sickness
Acetazolamide
Fomepizole indication
Methanol poisoning
Ethacrynic acid moa
Loop diuretic
Risk of otoxicity highest with which loop diuretic?
ETHACRYNIC ACID
Metolazone drug class
Thiazide diuretic
Thiazide diuretics have what effect on blood sugar and LDL?
Elevate
amiloride drug class
Potassium sparing diuretic
Best diuretic in PCOS
Aldactone
Drug of choice for central diabetes insipidus
Desmopressin
Major ADR with desmopressin
Water intoxication
Inhibition of conversion of angiotensin 1 to 2 causes blood pressure to lower how?
Lowers arteriolar resistance
Ace inhibitors contraindicated in renal artery ___
Stenosis
How does RAAS contribute to hypertension?
Volume overload, so body releases renin, which elevates angiotensin and aldosterone, leading to arteriolar contraction and elevated blood pressure.
Aliskiren moa
Direct renin inhibitor
With nitrates, need drug free interval of how long?
8 hours
2 indications for calcium channel blockers
Angina and HTN
Which formulation of calcium channel blocker preferred for angina?
Long acting or XR
Odd potential nifedipine side effect
Tachycardia
Common gi side effect with diltiazem and verapamil:
Constipation
4 unique and common side effects of beta blockers
Bronchospasm, peripheral vasoconstriction, depression, and worsening psoriasis
Ranolazine indication
Angina
Ivabradine moa
Decreases heart rate by inhibiting SA node firing
Ivabradine 2 indications
Heart failure and angina
Ivabradine visual side effect
Phosphene (perception of light when none entering eye)
Ivabradine contraindicated with what drugs?
Diltiazem or verapamil
Heparin moa
Thrombin and factor Xa inhibitor
Thiazides lose efficacy at what eGFR? 2 Exceptions:
<40, indapamide and metolazone
Which 3 beta blockers indicated for heart failure?
Nebivolol, metoprolol, and bisoprolol
2 Beta blockers of choice in peripheral artery disease
Coreg and labetalol
Isosorbide dinitrate and Hydralazine combo indication
Heart failure in African americans
3 digoxin common side effects
Nausea, diarrhea, visual disturbances
When is Ivabradine used in heart failure?
Not tolerating beta blockers or HR over 75 on a beta blocker
Quinidine indication
Prevent AF, VT, and VF
3 common side effects with quinidine
Diarrhea, QT prolongation, cinchonism: (tinnitus, blurred vision, flushing, dizziness, diarrhea)
Useful general info about theophylline dosing
Narrow therapeutic index
Disopyramide common side effects
Anticholinergic
Lidocaine systemic CNS side effects
Seizures, tinnitus, tremor, hallucinations, drowsiness, and coma
Mexiletine 2 indications
Chronic VT and VF prevention
Systemic lidocaine indications
Acute VT and VF treatment
Mexiletine common 2 side effects
Tremor and nausea
Lidocaine and Mexiletine MOA
Sodium channel blocker, fast wear off
Procainamide, quinidine, and disopyramide MOA:
Sodium channel blockers, intermediate wear off
Flecainide and propafenone MOA:
Sodium channel blockers, slow wear off
Which class of antiarrhythmics 1a, 1b, or 1c is best tolerated?
1c (flecainide)
Flecainide and propafenone increase risk of severe arrhythmia in what patient type?
Structural heart disease.
Flecainide increases mortality in what patient specific heart disease status?
MI
2 common side effects of flecainide:
Blurry vision and can worsen heart failiure
Additional mechanism for propafenone:
Beta blocker
What are class 2 antiarrhythmics?
Beta blockers
Nadolol preferred for what 2 specific heart disease states?
Long QT syndrome and CPVT (catecholaminergic polymorphic ventricular tachycardia) (genetic heart defect)
Drug of choice for acute VT and VF and to slow ventricular rate and convert A fib.
Amiodarone
Why does amiodarone use require periodic lung evaluation
Pulmonary fibrosis side effect
5 common amiodarone side effects:
Corneal deposits, hepatotoxicity, neuropathy, photosensitivity, thyroid dysfunction
Multaq indication
A fib prevention
Why use multaq?
Less side effects
2 common dronedarone side effects
GI disturbances and fatal hepatotoxicity
Multaq increases mortality in patients with severe:
heart failure
Sotalol, tikosyn, amiodarone , and ibutilide MOA:
Potassium channel blocker
Sotalol, tikosyn, and ibutilide have high risk for what side effect?
TDP
MOA of class 4 antiarrhythmics
Calcium channel blockers
4 common side effects of verapamil and diltiazem
Constipation, bradycardia, hypotension, and gingival hyperplasia
NDHP calcium channel blockers contraindicated in what?
Heart failure with reduced ejection fraction
Treat TDP with what?
Mag sulfate
Digoxin MOA
Sodium-potassium ATPase inhibitor
Digoxin indication
Rate control in a fib
Digoxin 3 common side effects
GI effects, arrhythmia, and visual/cognitive dysfunction
Avoid what 2 drug classes with Cialis and such
Nitrates and alpha inhibitors (amlodipine and clonidine…)
Riociguat indication
Pulmonary arterial hypertension
Drug class first line for severe PAH
Prostacyclin analogs
Treprostinil 5 side effects
Jaw pain, hypotension, myalgia, flushing, NV
When is dose adjustment required for lovenox?
Crcl less than 30
Warfarin moa
Vitamin k antagonist
How to adjust warfarin in renal or hepatic impairment:
None, watch INR
Dabigatran
Pradaxa
Pradaxa dose reduction at what Crcl:
30
When can xarelto be given twice daily?
VTE treatment and acute coronary syndrome
When to get reduced dose Eliquis?
2 of these: Older than 80, weight < 60 kg, or Scr >=1.5
Savaysa
Edoxaban
Savaysa moa
Factor Xa inhibitor
What drug can be used to reverse eliquis and xarelto?
Andexxa (andexanet alfa)
Alteplase indication
Thrombolysis
Dipyridamole moa
Inhibits platelet aggregation and causes coronary vasodilation
Brillinta indication
ACS
Effient indication
After intervention for ACS
Do not use prasugrel in what age
> 75
Reduce prasugrel dose at what weight?
<60 kg
Statin use in pregnancy
Contraindicated
Safest lipid lowering drugs
Bile acid sequestrants
3 Common side effects of bile acid sequestrants:
Bloating, constipation, dyspepsia
Contraindication to bile acid sequestrant use
Hypertriglyceridemia, these increase triglycerides
Why is niacin included in prenatal vitamins, but contraindicated in pregnancy?
18 mg in prenatals, but 500 mg in rx strength.
Niacin effect on HDL, LDL, and triglycerides
Increase, decrease, decrease
Rx niacin 3 common side effects
Flushing, dyspepsia, and itching
Niacin should not be used with what class of hyperlipidemia drugs
Statins due to myopathy
Niacin is contraindicated with what 2 diseases?
Hx of peptic ulcer disease, and gout
When to choose fibrates?
Hypertriglyceridemia
Can fibrates be used in pregnancy?
No
When can fibrates be used with statins?
They should not
2 Most common side effects with fibrates
GI and myopathy
When to use zeta and bile acid sequestrants together?
Never
Can PCSK-9 inhibitors and statins be used together?
Yes. Complementary mechanisms.
How do statins Lower LDL?
Inhibit LDL biosynthesis
PCSK-9 moa
Increases LDL receptors and therefore LDL cell uptake.
PCSK-9 2 common side effects:
Influenza symptoms and URTI’s
Omega-3 indication
Hypertriglyceridemia
3 common side effects with omega-3’s
Arthralgia, nausea, and dyspepsia
Xifaxan 4 common side effects
Nausea, dizziness, fatigue, and swelling
Xifaxan moa
Antibiotic DNA synthesis inhibitor
Prednisone effects on cellular immunity:
Decreases pro-inflammatory cytokines IL-1 and IL-6, decreases T cell proliferation, but increases neutrophil and monocyte function.
2 Less obvious cyclosporine indications:
Rheumatoid arthritis and psoriasis
Cyclosporine severe interactions with what drug class?
Antiarrhythmics
9 common side effects with cyclosporine systemic
Tremor, hallucinations, drowsiness, coma, nephrotoxicity, HTN, hirsutism, HLD, and gum hyperplasia
Cyclosporine and tacrolimus MOA
Calcineurin inhibitor (reduce T cell activity)
What lab with tacrolimus?
Blood levels to avoid tacrolimus
Azathioprine moa
Purine metabolism inhibitor
5 commons side effects with azathioprine
Bone marrow suppression, infection susceptibility, hepatotoxicity, alopecia, and gi toxicity
Mycophenolate moa
Purine metabolism inhibitor
Mycophenolate 2 common side effects
GI and hematologic.
Sirolimus which cyp interactions?
3A, watch interactions
Who not to use probiotics in?
Immunocompromised: risk of translocation and septicemia.
Sirolimus moa
Mtor inhibitor: inhibits cytokine mediated T cell proliferation.
Belatacept
Nulojix
Belatacept moa
T cell stimulation blocker
Belatacept only indication
Transplant rejection prevention
Belatacept dose dependent risk:
Dose dependent PML, CNS lymphoproliferative disorder, and CNS infections
What is ATGAM?
Antibodies against numerous T cell surface molecules.
ATGAM indications:
Prevention and treatment of transplant rejection and aplastic anemia
Alemtuzumab moa
Anti cd 52, lymphocyte depletion
Rituximab 2 indications:
RA and MS
Remicade moa
TNF inhibitor
Enbrel moa
TNF inhibitor
What 4 infusion reactions with humoral, Enbrel, and remicade?
Fever, urticaria, hypotension, dyspnea
3 risks with TNF inhibitors
Serious infections, lymphoma, and other malignancies
Name a first line option for MS
Ocrelizumab
Tecfidera indication
MS
Misoprostol alternative indication
GI acid protective
Epoprostenol drug class and indication
Prostacyclin analogue and pulmonary arterial hypertension
Bimatoprost common side effect vs other “prost” eye drops
Upper respiratory tract infection 10% incidence
Bimatoprost 2 indications:
Eyelash darkening and growth and ocular hypertension (glaucoma prevention and treatment)
Aspirin prolongs bleed time for how long after a dose?
36 hours
Aspirin associated Reye syndrome in kids is associated with what 2 symptoms/diagnoses?
Fever and flu or varicella disease
Diflunisal drug class
Salicylate
Diflunisal 2 indications
Osteo and rheumatoid arthritis
Why is mesalamine only used for IBD?
Specific to lower gi tract.
3 risk factors that lower threshold for Tylenol toxicity
Liver impairment, more than 2 alcohol drinks per day, and malnutrition
What is hepatotoxic acetaminophen metabolite?
NAPQI
What effect does Tylenol have on platelets and inflammation?
Little effect
NSAID used in patent ductus arteriosus in neonates
Indomethacin
Indomethacin high risk in what patient population?
Over 65 years old due to high incidence of side effects
Why is Indomethacin not used as much as other NSAIDS?
Lots of side effects 20% discontinue
Ketorolac effect as anti-inflammatory:
Little effect
Diclofenac common, severe side effect
Liver toxicity 4%
Mefenamic acid drug class
NSAID
Mefenamic acid 2 indications
Pain and dysmenorrhea
Mefenamic acid used in what age group and what max duration?
Over 14 and 7 days
Ibuprofen effect on aspirin cardioprotection
Reduces cardioprotection by competing with aspirin for cox binding site.
Oxaprozin drug class
NSAIDx
Oxaprozin half life
41-55 hours
Oxaprozin not indicated for what pain?
Acute, slow onset
Piroxicam half life
50 hours
Piroxicam 2 serious side effects and how common?
Serious GI and skin reactions, 5%
NSAID to use to avoid gi side effects
Celecoxib cox 2 selective
Colchicine moa
Depolymerizes microtubules, decreasing neutrophil migration into inflamed sites.
Which probiotics to use in C diff?
None recommended. Conflicting evidence.
Allopurinol secondary indication:
Calcium oxalate stones
In what impairment does allopurinol dose need to be adjusted?
Renal
Risk of ___ attacks during early allopurinol treatment.
Gout (tissue urate mobilization)
How long does allopurinol take to get Uris acid levels down to normal?
1 to 3 weeks
Allopurinol and febuxostat moa
Xanthine oxidase inhibitors
What is the most effective drug class for acute migraines?
Triptans (eletriptan), not CGRP’s
Main contraindication for triptans
Vascular disease (stroke, Coronary artery disease, heart attack hx, peripheral artery disease, CHF, pulmonary embolism hx…)
2 Probenecid indications
Hyperuricemia (not acute), elevated beta lactam levels
Probenecid moa
Uric acid reabsorption inhibitor in kidneys
Doxepin moa
tricyclic antidepressant
Doxepin topical cream indication
Itching
Pyrilamine moa
Combo topical Antihistamine
Promethazine boxed warning
Fatal respiratory depression under 2 years old
Bepotastine drug class
Ocular antihistamine
Epinastine drug class
Ocular antihistamine
Albuterol 4 major side effects
Tachycardia, palpitations, muscle tremors, hyperkalemia
Levalbuterol advantage over albuterol
None
How is Formoterol used in asthma?
Combo with ICS
Loose contraindication for patients on SAMA or LABA?
Urinary retention and glaucoma
ICS 2 local side effects
Hoarseness and thrush
Which ICS ideal in children?
Budesonide
Montelukast moa
Leukotriene antagonist
Zileuton drug class
Leukotriene antagonist
What elevated lab contraindicates zileuton?
ALT / AST
Theophylline / aminophylline 5 commons side effects
Nausea, headache, diuresis, arrhythmia, seizure
Roflumilast moa
PDE-4 inhibitor: inhibits WBC infiltration of lung cells to prevent remodeling and elevates cAMP in lung cells
Omalizumab 4 indications:
Allergic asthma, food allergy (ig-E mediated), rhinosinusitis w/polyps, chronic urticaria
Xolair moa
Anti- ig-E
Dupixent moa
IL-4 antagonist
Dupixent 7 indications:
Moderate to severe eosinophilia asthma or ICS dependent, asthma with mod to severe atopic dermatitis, atopic dermatitis mod-severe, refractory COPD, eosinophilia esophagitis, prurigo nodularis, and sinusitis w/polyps
Generic growth hormone drug name
Somatropin
Leydig cell function
Stimulate testosterone production in the testes
Octreotide moa and indication
Somatostatin analog (inhibits growth hormone secretion) and acromegaly
Cabergoline moa and 3 indications
D2 agonist, hyperprolactinemia, Parkinson’s, and acromegaly
Which thyroid hormone is active? T3 or T4?
T3
Getting a thyroid dose that is too high can lead to what 2 diseases?
Osteoporosis and atrial fibrillation
Armour thyroid composition
T3 and T4
Methimazole and PTU moa
Reduce thyroid hormone production by interfering with iodine incorporation into tyrosyl residues
Methimazole pregnancy use:
Not first trimester due to embyopathy
Major concern with propylthiouracil:
Liver toxicity
What drug can be used for hyperthyroidism in the first trimester?
PTU
Lugol solution indication
Reduce secretion and synthesis of thyroid hormone
Lugol solution dose in thyroid storm in pregnancy:
Contraindicated
SSKI indication
Acute thyroid secretion and synthesis inhibition
Tamoxifen moa and indication
SERM, breast cancer treatment
Raloxifene moa and 2 indications
SERM, osteoporosis treatment, breast cancer prophylaxis in high risk post-menopausal women
SERM 2 major side effects
Hot flashes and clots
Clomiphene moa
Anti estrogen
Exemestane moa and indication
Irreversible aromatase inhibitor, breast cancer treatment
Anastrozole and letrozole moa and indication
Reversible aromatase inhibitor. Breast cancer treatment.
Risk with long term use of aromatase inhibitors:
Osteoporosis
Megestrol is a derivative of what naturally occurring hormone?
Progesterone
What activity differentiates norethindrone from other progestins?
Androgenic activity
Mifepristone moa
Both progesterone receptor antagonist.
Leuprolide moa and 2 common indications
GnRH agonist, reducing GnRH secretion, and therefore testosterone and estrogen. Endometriosis, precocious puberty
Leuprolide long term use side effect
Osteoporosis
What options exist outside clomiphene for ovulation induction?
injectable FSH and LH
Bicalutamide moa and indication
Androgen receptor antagonist, add on for metastatic prostate cancer
Finasteride moa and indications
5 alpha reductase inhibitor, reduces production of dihydrotestosterone in prostate, shrinking the prostate. Alopecia and BPH
Sildenafil moa and indications
PDE-5 inhibitor(allows relaxation of cavernosal smooth muscle), ED and pulmonary arterial hypertension
PDE-5 inhibitor DDI contraindication
Nitrates
3 common side effects with PDE-5 inhibitors:
Headache, flushing, and blue-green tinted vision
Chronic hydrocortisone dosing tip: AM and PM doses
20 mg AM, 10 mg PM for sleep
Fludrocortisone dose is titrated up by what? How often dosed?
Blood pressure (upright posture tolerance) once daily due to long half life
Corticosteroid 3 short term side effects:
Insomnia, weight gain, emotions
High-dose/long term corticosteroid 6 side effects:
Psychosis, infection risk, osteoporosis, osteonecrosis, myopathy, HPA axis suppression
2 common side effects of steroid eye drops:
Glaucoma and cataract formation
Chronic inhaled steroid use in children effect on height:
Slow growth velocity, no effect on final height.
inhaled steroid with least side effects and why:
Ciclesonide, low oral biavailability
Reasons for steroid use in leukemia and lymphoma
Cytotoxic effects and relief of pain, nausea, and appetite stimulation
Cabergoline off label use for reduction of ACTH
Cushing disease
Regular insulin onset and duration
30 minutes, 4-6 hours
Rapid acting insulin onset and duration
10 minutes, 3-4 hours
NPH insulin onset and duration
1 hour, 8-12 hours
Long acting insulin onset and duration
1 hour, 18-42 hours (Degludec 42 hours)
Metformin moa
Increase glucose uptake peripherally, decrease hepatic gluconeogenesis
3 common ADR’s with metformin
Nausea, diarrhea, and lactic acidosis
Why metformin stopped on hospital admit?
Contrast dye elevated levels due to renal insult
Is metformin used in renal and hepatic problems?
Dose adjust for renal, not in liver problems
Acarbose drug class and moa
Alpha glucose dose inhibitor, reduces carb breakdown in gi tract.
2 common side effects with acarbose
GI flatulence and elevated LFT’s
Name 2 DPP4’s
Sitagliptin, saxagliptin, linagliptin, alogliptin
DPP4 moa
Inhibit breakdown of GLP-1, increased satiety, lower blood glucose.
Name the 3 sulfonylureas
Glipizide, glimepiride, glyburide
Sulfonylurea moa
Stimulate insulin release
Sulfonylurea major side effect
Hypoglycemia
Nateglinide and repaglinide moa
Increase insulin secretion
Jardiance class and moa
SGLT2 inhibitor. Decrease glucose reabsorption in kidneys.
Main side effect of SGLT2 inhibitors:
Increased risk of UTI
What serious diabetes complication can SGLT2 inhibitors mask?
DKA
What side effect do SGLT2 inhibitors not cause that other diabetes drugs do?
Hypoglycemia
Actos moa
Increase peripheral insulin sensitivity
5 common side effects for actos:
Edema, CHF, weight gain, fractures, macular edema
Actos drug class
Thiazolidinedione
actos absolutely contraindicated in:
CHF reduced ejection fraction
GLP-1 agonists 5 common side effects:
Nausea, GI, headache, fatigue, sinus infection
Avoid using GLP-1’s with agents that do what?
Decrease GI motility (oxybutynin…)
Pramlintide moa
Slows gastric emptying and decreases glucagon (like amylin naturally occurring)
Diazoxide moa
Inhibits insulin secretion
Name 3 Diazoxide common side effects
Nausea, edema, hyperuricemia, thrombocytopenia, hypertrichosis (hair growth), leukopenia
Diazoxide 2 indications
Hypertensive crisis, hyperinsulinemia
Octreotide common side effect
Gallbladder abnormality
Parathyroid hormone effect on calcium
Release calcium from bone into bloodstream, increase gastric calcium absorption, decrease renal excretion of calcium, stimulate osteoblasts.
Why would vitamin d help with hypoparathyroidism?
Low blood calcium from low absorption leads to hypoparathyroidism and osteoporosis, so vitamin d helps with calcium uptake and parathyroid hormone secretion
Why would vitamin d help with CKD induced hyperparathyroidism?
Parathyroid is released to increase blood levels of calcium, depleting bone stores (osteoporosis). Vitamin d increases absorption of calcium.
Calcitriol moa
Active form of vitamin d for CKD patients.
Calcitriol effect on phosphate
Elevate levels of phosphate
Hyperphosphatemia effects in body
Calcium deposits in heart, liver, kidneys… muscle cramps
Hypophosphatemia body effects
Fatigue, weakness, bone pain, seizures (acute re-feeding)
Phosphate actions in body:
Converting ADP to ATP, bone mineralization, glycolysis, component of cell membrane and DNA and RNA, effects oxygen-carrying capacity of hemoglobin, and acts as urinary buffer by binding to free hydrogen ions.
First line option for reducing dietary phosphate
Tums
Rx option for phosphate binding
Sevelamer carbonate
Bisphosphonate moa
Reduce osteoclast activity, allowing bones to stay strong
Counseling point on bisphosphonates:
Take on empty stomach and sit up 30 minutes after dose (esophageal ulcers).
2 severe issues with bisphosphonates
Osteonecrosis of the jaw and femoral fractures
Bisphosphonates are contraindicated with delayed ___ ___
Esophageal emptying
When to change dose or switch from ibandronate.
Poor kidney function (CrCl under 30)
Zoledronate contraindicated in what 2 things?
CrCl under 35 and hypocalcemia
Forteo
Teriparatide
Forteo use limited to less than ___
2 years
Forteo moa
Parathyroid hormone analog (stimulates osteoblasts, increases gastric absorption of calcium, inhibits calcium excretion via kidneys)
Chronic high parathyroid hormone net effect
Osteoporosis
Pulse dosing of parathyroid hormone net effect
Bone building
Hormone that works opposite of parathyroid?
Calcitonin
Cinacalcet moa
Calcium sensing receptor mimetic (tells sensor that calcium level too high)
Cinacalcet 2 indications
Hypercalcemia and secondary hyperparathyroidism of CKD.
Side effect of cinacalcet
Hypocalcemia
Cinacalcet interactions:
Cyp3a4 strong inhibitors and CYP2d6 substrates.
Calcitonin effect on osteoclast
Inhibitor.
Denosumab moa
Binds to RANKL, blocks interaction between RANKL and RANK on osteoclast surface, and prevents osteoclast formation. Builds bone mass.
Hydrochlorothiazide effect on calcium
Reduce calcium excretion
Potentially serious DDI with omeprazole
Plavix, studies show increased mortality risk, some studies did not show risk. Better to avoid.
4 PPI side effects:
Fracture risk, diarrhea, nephritis, b-12 deficiency (long term 3 years use)
Misoprostol side effect
Diarrhea
Sucralfate side effect
Constipation
Prucalopride moa
5ht-4 agonist, increase GI motility
Prucalopride 3 indications
GERD, gastroparesis, severe constipation
2 side effects and 1 risk of prucalopride
Headache and diarrhea. Serious cardiac risk
Mechanism of gastric movement by metoclopramide:
5HT4 agonist
3 side effects of metoclopramide:
hyperprolactinemia (dopamine antagonism induced), CNS depression, and EPS (tar dive dyskinesia)
What macrolide increases gastric motility?
Erythromycin
Lactulose 2 indications:
Constipation and hepatic encephalopathy
Linzess youngest age for use:
6 years old
Linzess moa
Guanylate cyclase-C agonist (draw water into bowel)
Lubiprostone moa
Cl channel activator (draw water into bowel)
2 lubiprostone side effects
Nausea and diarrhea
Naloxegol moa
Mu opioid receptor antagonist peripherally for constipation
Alosetron indication
IBS-D (women)
Preferred antibiotic for children with traveler’s diarrhea
Azithromycin
Xifaxan 2 indications
Traveler’s diarrhea and IBS-D
What type of diarrhea does clonidine help with?
Diabetic diarrhea
Lomotil and loperamide soft duration limit
10 days.
Dicyclomine 3 contraindications
Colitis, bowel obstruction, and GERD
Zofran moa
5HT3 antagonist
Ondansetron 4 common side effects
Headache, constipation, fatigue, malaise
How does prochlorperazine inhibit nausea?
Dopamine antagonism at chemoreceptor trigger zone.
How does scopolamine inhibit nausea?
Anti muscarinic that blocks histamine signals from inner ear to vomiting center
5 common side effects with scopolamine
Dizziness, constipation, drowsiness, dry mouth, blurred vision
Ursodiol indication
Prevention and dissolution of gall stones
Ursodiol 2 side effects
Nausea (GI) and headache
Mesalamine by mouth has less effects where in GI tract?
Ileum and large intestine
How does sulfasalazine reach distal regions of GI tract?
Prodrug metabolized by colonic bacteria.
Why balsalazide?
Reaches colon and does not contain sulfa group.
Big risk of IBD treatment with 6 mercaptopurine
4 fold higher risk of lymphoma
Big risk of treatment with azathioprine
4 fold risk of lymphoma
What 2 antibiotics are commonly used together in pediatric Crohn’s disease? Not effective in what?
Cipro and flagyl, Ulcerative colitis
Positional counseling point for doxycycline and all tetracyclines:
Do not recline for 1 hour after taking orally due to esophagitis risk.
Metronidazole 2 common side effects
Headache and metallic taste (dysgeusia)
First line in giardiasis
Metronidazole
What is used for resistant giardiasis?
Nitazoxanide
Drug of choice in trichomoniasis
Metronidazole
3 drug regimen for toxoplasmosis:
Pyrimethamine, sulfadiazine, and leucovorin.
Drug of choice for cryptosporidiosis
Nitazoxanide
What is albendazole used for?
Intestinal worms.
Sulfa antibiotics: bactericidal or static?
Static, folate synthesis inhibitor.
How does silver sulfadiazine work?
Prevents infection via folate synthesis inhibition
Bactrim has excellent efficacy against what 4 bugs?
Staph aureus, staph epi, strep pyogenes, and e. Coli
3 common side effects of bactrim
Rash, GI upset, and hyperkalemia
Quinolones: cidal or static?
Cidal
Quinolone moa
DNA storage damage, inhibit dna topoisomerase and gyrase
Do not give quinolones with:
Divalent cations
3 common side effects with quinolones
Neuro, tendinitis, and photosensitivity
Quinolones are typically avoided in what 2 patient types?
Pregnancy and children
Cipro has excellent coverage of what 6 bugs?
E. Coli, klebsiella, proteus, serratia, salmonella, shigella
Levaquin has excellent coverage of bugs of cipro and which 4 additional bugs?
Strep, H flu, legionella, and chlamydia
Moxifloxacin cannot be used for what infection?
UTI, no penetration
Methenamine moa
Forms formaldehyde in urine, chronic suppression of UTI
Methenamine requires ___ urine to work
Acidic
Nitrofurantoin moa
Causes DNA damage to bacteria.
3 things to watch out for with nitrofurantoin
Pulmonary toxicity, peripheral neuropathy, and turns urine brown
Does fosfomycin have effect in blood?
No, only urine
Fosfomycin moa
Inhibits cell wall synthesis
What drug for UTI with proteus?
Fosfomycin
Are penicillins cidal or static?
Cidal
Dicloxacillin indications
Skin and soft tissue MSSA infections
Amoxicillin and ampicillin have excellent coverage of what 2 bugs?
Beta hemolytic strep and E. Faecalis
Augmentin adds excellent coverage of what 3 bugs?
B. Frag, H flu, and proteus
Cefadroxil what gen cephalosporin?
1st gen
Cephalexin and cefadroxil cover what 2 bugs excellently?
MSSA and streptococci
Cefuroxime, cefaclor, and cefprozil what gen?
2nd gen
2nd gen cephalosporins add coverage of what bugs?
H flu, proteus, E. coli, klebsiella
Cefpodoxime what gen?
3rd gen
Cefixime what gen?
3rd gen
Third gen cephalosporin 5 indications:
CAP, meningitis, UTI, strep endocarditis, and gonorrhea
Aminoglycosides cidal or static?
Cidal
Aminoglycoside moa
Concentration dependent, Inhibit bacterial protein synthesis
Aminoglycoside oral absorption
Almost none, only used orally for bowel decontamination
Ear administration of aminoglycosides should be avoided in what patients?
Those with tubes in (ototoxicity)
Tetracycline moa
Protein synthesis inhibitor
Tetracyclines: cidal or static?
Static
Why tetracyclines avoided in pregnancy and children under 8?
Binds to developing bone and causes malformations
Tetracyclines time or concentration dependent?
Time
Macrolide moa
Inhibit bacterial protein synthesis
Macrolide: cidal or static? Time or concentration dependent?
Static, concentration
Which macrolides are major cyp inhibitors?
Erythromycin and clarithromycin
Claithromycin usually seen in what 2 infections?
H pylori and CAP
Clarithromycin side effect at high doses
Tinnitus
Azithromycin half life
48 hours
When would you see telithromycin?
Macrolide resistant strep and staph
Why is telithromycin not used often?
Severe Hepatotoxicity
Clindamycin moa
Protein synthesis inhibitor
Clindamycin good activity against what bug class?
Strep (pyogenes, pneumo, and viridans)
Linezolid moa
Static protein synthesis inhibitor
Linezolid DDI
SSRI, serotonin syndrome
Why is Linezolid not dosed once daily?
Time dependent
Vancomycin, cidal or static? Moa
Cidal cell wall synthesis inhibitor
Oral vancomycin indication:
C diff
Is oral vancomycin absorbed?
No
Daptomycin not effective for what site?
Lungs (pneumonia), inactivated by lung surfactant
Daptomycin moa
Cidal cell wall synthesis inhibitor
Metronidazole moa
Disrupt dna synthesis in anaerobes
Metronidazole has good coverage of what 2 species?
B frag and clostridium
Bacitracin and mupirocin moa
Cell wall synthesis inhibitor
Rifampin general ddi
Potent Cyp inducer
Why is rifampin a problem in alcoholics?
Hepatitis
Tuberculosis treatment acrostic
RIPE (rifampin, isoniazid, pyrazinamide, ethambutol)
Dapsone topical indication
Acne
Dapsone moa
Folate antagonist
Dapsone oral 4 common indications
Leprosy, malaria in combo, pneumocystis jiroveci, toxoplasma prophylaxis
What test prior to using dapsone
G6PD deficiency
Dapsone can cause what side effect at 200+ mg per day dose?
Hemolysis
Azole antifungal moa
Ergosterol synthesis inhibition
Itraconazole potent ddi
Cyp 3A4 inhibitor
Fluconazole inhibits what 2 cyps?
3a4 and 2c9
Posaconazole administration
With food
What drug for mucormycosis?
Isavuconazole
Griseofulvin moa and 2 indications
Inhibits microtubule function, ringworm and toenail fungus
Griseofulvin has what effect on cyp’s?
Induction
Terbinafine moa and 2 indications
Inhibit fungal squalene epoxidase and reduce ergosterol synthesis. Ringworm and toenail fungus
Terbinafine ____ in skin, nails, and fat
Accumulates
Acyclovir and Val limited to use in ____ viruses
Herpes
Best against cytomegalovirus
Valgancyclovir
Trifluridine indication
Ocular herpes
Oseltamivir moa
Neuraminidase inhibitor, prevents release of complete virus from cell.
Amantadine moa as antiviral
Inhibits m2 protein function
Entecavir moa
Inhibits HBV reverse transcriptase
Entecavir counseling point administration
Empty stomach
Tenofovir disoproxil fumarate moa
Reverse transcriptase inhibitor
Tenofovir 6 common side effects:
Abd. Pain, nausea, insomnia, pruritus, dizzyness, pyrexia
Lamivudine 2 common side effects
ENT infections and diarrhea
Sofosbuvir/velpatasvir indication
Hep c treatment (all genotypes)
Velpatasvir administration
Acidic stomach required
Avoid sofosbuvir if Crcl under ___
30
2 common side effects of sofosbuvir/velpatasvir
Fatigue and headache
Sofosbuvir moa
Inhibits HCV RNA polymerase
Difference between NRTI and NNRTI meds
NNRTI’s are newer and do not require phosphorylation to be activated, NNRTI’s are not active against HIV-2
Zidovudine 3 common side effects:
Anemia, neutropenia, and myopathy
Lamivudine 2 indications:
HBV and HIV
Lamivudine clinical pearl about side effects:
Essentially non toxic
Abacavir side effect to watch for
Hypersensitivity syndrome: fever, abd. Pain, and rash associated with HLA B*5701, stop use: potentially fatal
Tenofovir 3 indications:
HIV treatment, HBV, and HIV prophylaxis
Tenofovir 2 unique side effects:
Nephrotoxicity (severe is rare) and bone mineral density loss with chronic use
Emtricitabine side effect clinical pearl
Generally non toxic
Difference between HIV-1 and 2:
HIV-2 is slower onset, HIV-1 is predominant in America.
Nevirapine drug class
NNRTI
Nevirapine clinical pearl
Autoinducer of metabolism
Nevirapine most common side effect:
Rash (resolves in time)
Efavirenz common side effect
CNS toxicity (resolves in time, but can be severe enough to stop drug)
Rilpivirine counseling point
Give with food, avoid PPI
Etravirine common side effect
Rash that resolves
Ritonavir moa
Protease inhibitor, potent CYP3A4 inhibitor (boosts concentration of other drugs)
Ritonavir common side effect
Nausea
Fosamprenavir drug class
Protease inhibitor
Loping if drug class
Protease inhibitor
Atazanavir drug class and co-administered with
Protease inhibitor, ritonavir or cobicistat
Darunavir drug class
Protease inhibitor
Darunavir co administration
Must be used with ritonavir or cobicistat
Best tolerated protease inhibitor in HIV
Darunavir
Drug class for maraviroc and enfuvirtide:
Cell entry inhibitors HIV
Drug class ending in “gravir”
Integrase inhibitors
Avoid taking integrase inhibitors with what?
Divalent cations
Integrase inhibitor counseling point on side effects
Well tolerated
3 drug classes in oncology:
Alkylating agents and platinum coordination complexes, antimetabolites, and natural products
Alkylating agents and platinum coordination complexes MOA:
Covalent modification of DNA (damage)
Alkylating agents and platinum coordination complex 5 side effect types:
Immunosuppression, dividing mucosal and hair follicle cell toxicity, delayed pulmonary fibrosis, reproductive system toxicity, leukemogenesis (leukemia causing)
Mechlorethamine drug class:
Alkylating agent
Cyclophosphamide drug class
Alkylating agent
Methotrexate drug class:
Antimetabolite
Carboplatin drug class
Platinum coordination complex
Pemetrexed drug class
Antimetabolite
5-fluorouracil drug class
Antimetabolite
Oxaliplatin drug class
Platinum coordination complex
Ifosfamide drug class
Alkylating agent
Melphalan drug class
Alkylating agent
Chlorambucil drug class
Alkylating agent
Capecitabine drug class
Antimetabolite
Cytarabine drug class
Antimetabolite
Bendamustine drug class
Alkylating agent
Busulfan drug class
Alkylating agent
Gemcitabine drug class
Antimetabolite
5-azacytidine drug class
Antimetabolite
Carmustine drug class
Alkylating agent
Streptozocin drug class
Alkylating agent
Procarbazine drug class
Alkylating agent
Dacarbazine drug class
Alkylating agent
Temozolomide drug class
Alkylating agent
Cisplatin drug class
Platinum coordinating complex
Mercaptopurine drug class
Antimetabolite
Fludarabine drug class
Antimetabolite
Antimetabolite moa
Inhibit DNA and RNA function and formation.
Vinblastine drug class
Natural products
Vinorelbine drug class
Natural products
Vincristine drug class
Natural products
Cladribine drug class
Antimetabolite
Eribulin drug class
Natural products
Paclitaxel drug class
Natural products
Docetaxel drug class
Natural products
Clofarabine drug class
Antimetabolites
Topotecan drug class
Natural products
Irinotecan drug class
Natural products
Nelarabine drug class
Antimetabolite
Actinomycetes drug class
Natural products
Daunorubicin drug class
Natural products
Doxorubicin drug class
Natural products
Pentostatin drug class
Antimetabolites
Mitoxantrone drug class
Natural products
Etoposide drug class
Natural products
Teniposide drug class
Natural products
What 2 non cancer indications does mercaptopurine have?
Crohn’s and ulcerative colitis
Hydroxyurea moa
Inhibits conversion of ribo to deoxyribonucleotides (inhibits DNA synthesis)
L-asparaginase moa
Deprives leukemia cells that lack asparagine synthase.
Bleomycin moa
Binds to DNA and causes damage.
EGFR function
Growth and differentiation of epithelial cells
EGFR tyrosine kinase inhibitor function
Inhibit function of EGFR
Monoclonal antibody targeting EGFR function
Reduce expression and function of EGFR, draw in immune cells to kill cell.
Sunosi moa
Dopamine and norepinephrine reuptake inhibitor. Does not cause monoamine release like adderall.
Drug ending in Mumab?
Humanized monoclonal antibody
Drug ending in Zumab?
Human protein with antigen biding region from mouse
Drug ending in Ximab?
Chimera of human constant and mouse variable antibody domains
Drug ending in Omab?
Fully mousey protein sequence
Drug ending in ib?
Small molecule drugs, mostly tyrosine kinase inhibitors.
What is HER2?
Human epidermal growth factor receptor 2, a common receptor that gets over expressed in breast cancers and can lead to more aggressive tumors.
Jak inhibitors moa
Reduce signaling for growth factors in hematopoeisis and immune cells
CDK4/6 inhibitor moa
Prevent cell progression through mitosis
BTK inhibitor moa
Prevents excessive B cell growth and differentiation.
BCR-ABL inhibitor drug name and importance
Gleevec (imatinib), prevents this BCR-ABL complex from forming and causing uncontrollable cell division.
ALK inhibitor moa
Prevent ALK (a protein in cell membrane) from forming oncogenic drivers
Inhibitor of PI3K/Akt/mTOR pathway moa
Excessive signaling through this pathway is common in many cancers, these promote cell death for out of control growth.
Why target VEGF in cancer?
To prevent tumor cells from hijacking blood flow and nutrients to support tumor growth.
Describe immune checkpoint inhibitors
Cancer cells down regulate T cells to promote their own survival, but the discovery of checkpoints that cancer cells use enabled inhibitors that allow T cells to stay active and kill cancer cells.
Name 3 checkpoint targets for inhibition
CTLA-4, PD-1 and PD-L1
Which interleukin is mimicked with drugs to fight cancer? MOA
IL-2, promotes T cell and NK cell growth, stimulates B cell proliferation and antibody production. Drives development of T regs (mediates tolerance and suppression). Limits dangerous autoimmune reactions.
Do cancer vaccines exist?
Technically yes, but they work for treatment, not prevention.
Explain moa of chimeric antigen receptor T cells: (CAR-T)
CAR-T cells have an engineered antigen receptor on the T cell surface that recognizes the specific cancer cell, then activates T cells to kill it.
Why target PARP1, a DNA repair enzyme?
Prevents cancer cells from repairing DNA, then they die faster than normal cells.
BCL2 target rationale
Family of proteins on cell membrane surface that control membrane permeability and apoptosis. BCL2 is like a dam that holds back apoptotic protein activation in cancer cells. Inhibition leads to cell death.
Thalidomide cancer use:
Inhibits growth and differentiation of multiple myeloma cancer cells, angiogenesis inhibitor, T cell activation.
Proteasome inhibitor moa in cancer
Disrupts intracellular signaling cascades and leads to apoptosis.
Moa of CD-20 inhibitors
All B cells express this receptor, causes death of B cells, useful in lymphomas with B cell hyper differentiation.
CD-52 targeting moa
CD-52 is an antigen expressed on neutrophils, and all B and T cells. This causes cancer cell death via antibody flagging mechanisms.
CD-33 target MOA
Expressed on many hematopoetic cancer cells, once taken into cell, potent toxin bound to drug kills cell.
Can Linzess caps be opened?
Yes, sprinkle on applesauce or water.
How is Clindamycin - benzoyl peroxide gel stored in pharmacy. At home?
Fridge, then room temp for up to 10 weeks
Why Briviact vs levetiracetam?
Significantly less side effects
Why is it a breakthrough to have colony stimulating factors available for erythrocytes, granulocytes, and macrophages in cancer?
This enables use of higher dose chemo drugs and the CSF’s help prevent febrile neutropenia and other associated immunodeficiencies.
Why is histone deacetylase a cancer target?
Inhibiting this family of enzymes can lead to prevention of differentiation in cancer cells (turned off at the genetic level).
Prednisolone max daily dose for acute disease in kids under 12:
60 mg
Tamoxifen moa
Selective estrogen receptor modulator, reduces estrogen levels and treats breast cancer. Both agonizes and antagonizes estrogen receptor.
Steady state tamoxifen levels reached how long? Why?
3-4 weeks, long half life
4 Possible tamoxifen major toxicities (2 agonist, 2 antagonist):
Agonist: endometrial cancer and clots.
Antagonist: vasomotor symptoms and menstrual irregularities
Fulvestrant moa difference from tamoxifen:
estrogen receptor downregulator, no agonist activity or side effects.
Anastrozole moa
Aromatase inhibitor, lowers serum estrogen
Letrozole moa
Aromatase inhibitor
Aromatase inhibitors contraindication:
Use in premenopausal women with ovarian function
Beyond use date for long acting inhalers? Same as expiration date?
90 days from opening seal, no.
Aromatase inhibitor 4 common side effects
Vasomotor (hot flashes, night sweats, palpitations), arthralgia, BMD loss (and osteoporosis and fractures), vaginal dryness (dyspareunia)
Megestrol moa
Progesterone receptor agonist
Megestrol 8 common side effects
Weight gain, nausea, vomiting, edema, breakthrough bleeding, SOB, thrombophlebitis (clot associated with vein inflammation), pulmonary embolism
Medroxyprogesterone cancer use:
Endometrial and breast cancers
4 common medroxyprogesterone side effects:
Hot flashes, weight gain, depression, amenorrhea
Leuprolide moa and indications
Gonadotropin releasing hormone agonist: androgen deprivation in advanced prostate cancer and breast cancer (suppress estrogen and progesterone production)
Bicalutamide indication and moa
Non steroidal anti androgen in castration resistant prostate cancer.
Bicalutamide 7 common side effects
Sexual dysfunction, gynecomastia, fatigue, diarrhea, headache, muscle pain, vasomotor.
Perphenazine class and moa
1st gen antipsychotic, D2 antagonist
Abiraterone moa and indication
Inhibit sex hormone production, treatment of advanced prostate cancer
Counseling point with abiraterone
Take on empty stomach, food causes increased concentrations and toxicity
Stimulation of what ophthalmic adrenergic receptor causes mydriasis?
alpha 1
Stimulation of what ophthalmic cholinergic receptor causes miosis?
M3
Name 1 anesthetic eye drop
Tetracaine or proparacaine
Durezol indication and moa
Pain and inflammation. Glucocorticoid
Which 2 steroid creams are considered high potency?
Clobetasol and betamethasone propionate
Limit topical steroids to what duration?
2-3 weeks
Avoid concurrent application of topical retinoids with what? And why?
DEET, due to increased DEET absorption. (Separate by 30 minutes)
How to start topical retinoids to avoid skin irritation
Every other night administration
Retinoids have decreased activity in the presence of what 2 things?
Sunlight and BPO
Which to retinoids do not have decreased activity if exposed to the above things?
Adapalene and tazarotene
Pregnancy should be avoided for how long after stopping isotretinoin?
1 month
Pregnancy should be avoided for how long after stopping acitretin?
3 years
6 non skin side effects of isotretinoin:
Conjunctivitis, myalgia, arthralgia, epistaxis, decreased night vision, and hyperlipidemia
Calcipotriene indication
Psoriasis
TNF inhibitor moa in psoriasis (3)
Reduces inflammation, decreases keratinocyte proliferation, and decreases vascular adhesion
Calcipotriene moa
Vitamin d analog that slows production of skin cells
Calcipotriene potential side effect:
Kidney stones
Azelaic acid 3 moa’s and 2 indications
Prevents clogged pores (comedolytic), antibiotic, anti-inflammatory for acne and rosacea
Why use Clindamycin with benzoyl peroxide?
Prevent resistance and better efficacy
Avoid what topical med with dapsone?
Benzoyl peroxide (orange-brown staining of skin/hair)
Why is erythromycin used with BPO?
To avoid bacterial resistance and have greater efficacy
Sulfur skin moa
Keratolytic
Sulfacetamide with BPO counseling point
Orange brown staining of clothes, not skin
Can neosporin be used in a surgical wound?
Not typically
Mupirocin used against which 2 bugs?
Staph aureus and strep pyogenes
Can topical ivermectin be used for scabies?
No, oral only
Moa for ivermectin against scabies and lice
Binds glutamate-gated chloride channels, causing hyperpolarization of nerve or muscle cells
Lindane indications:
Scabies and lice
Malathion indication and moa
Head lice, acetylcholinesterase inhibitor (causing paralysis)
Permethrin indicated for as young as what age?
2 months
3 skin indications for dapsone:
Dermatitis herpetiformis (recurrent skin rash autoimmune), leprosy, neutrophilic dermatoses
Podofilox indication
Genital warts
Imiquimod moa and 3 indications
TLR-7 activator, inducing cytokines and upregulating immune response. Genital warts. Actinic keratoses, superficial basal cell carcinoma
Topical urea moa
Hydration, enhancing skin peeling
Topical sulfur moa in hyperkeratotic disorders
Breaks down keratin by binding with cysteine and reducing to hydrogen sulfide
Penicillamine indication
Copper poisoning
Indication for deferoxamine, deferasirox, and deferiprone
Acute and chronic iron toxicity
