Pharmacy Foundations Part 1

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Primary NT of sympathetic nervous system

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Norepinephrine (NE) and Epinephrine (EPI)

- Bind to adrenergic alpha and beta receptors

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Primary NT of parasympathetic nervous system

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ACh (acetylcholine)

- Bind to muscarinic receptors

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224 Terms

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Primary NT of sympathetic nervous system

Norepinephrine (NE) and Epinephrine (EPI)

- Bind to adrenergic alpha and beta receptors

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Primary NT of parasympathetic nervous system

ACh (acetylcholine)

- Bind to muscarinic receptors

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Primary NT of somatic nervous system

ACh (acetylcholine)

- Bind to nicotinic receptors

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Catecholamine Metabolism

Breakdown Facilitated By MAO:

Tryptophan -> 5-HT -> metabolites

Tyrosine -> DOPA -> Dopamine -> NE -> EPI

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Neutral Functional Groups

Hydroxyl or alcohol (primary)

Ketone

Aldehyde

Amide

Nitrate

Nitro

Aromatic (benzene) ring

Urea

Carbonate

Carbamate

Ether

Thioether

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Acidic Functional Groups

Carboxyl

Phenol

Imide

Sulfonamide

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Basic Functional Groups

Amine (primary)

Amine (tertiary)

Imine

Amidine

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Amoxicillin Drug Structure

Beta-lactam fused to 5-sided ring

<p>Beta-lactam fused to 5-sided ring</p>
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Ceftriaxone Drug Structure

Beta-lactam fused to 6-sided ring

<p>Beta-lactam fused to 6-sided ring</p>
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Ertapenem Drug Structure

Beta-lactam fused to 5-sided ring

<p>Beta-lactam fused to 5-sided ring</p>
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Aztreonam Drug Structure

Beta-lactam ring not fused to another ring

- Monobactam

- Not cross reactive with other abx

<p>Beta-lactam ring not fused to another ring</p><p>- Monobactam</p><p>- Not cross reactive with other abx</p>
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Gentamicin Drug Structure

Amine group (amino) and a sugar (glycoside) group

<p>Amine group (amino) and a sugar (glycoside) group</p>
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Sulfamethoxazole Drug Structure

Contains a sulfonamide group

- Cross-reactive with celecoxib

<p>Contains a sulfonamide group</p><p>- Cross-reactive with celecoxib</p>
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Aspirin Drug Structure

Has an acidic carboxyl group

<p>Has an acidic carboxyl group</p>
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Ibuprofen Drug Structure

Has a carboxyl group

<p>Has a carboxyl group</p>
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Amphetamine Drug Structure

Contains a primary amine functional group

<p>Contains a primary amine functional group</p>
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Levothyroxine Drug Structure

Has 4 iodine molecules (T4 thats converted to T3)

<p>Has 4 iodine molecules (T4 thats converted to T3)</p>
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Amiodarone Drug Structure

Has 2 iodine molecules

<p>Has 2 iodine molecules</p>
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Fenofibrate Drug Structure

Contains ketone groups

<p>Contains ketone groups</p>
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Amitriptyline Drug Structure

Three rings in it

<p>Three rings in it</p>
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Chlorpromazine Drug Structure

Contains a thioether group

<p>Contains a thioether group</p>
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Drug Degradation: common chemical reactions that cause them to become unstable and degrade

Hydrolysis (water causes cleavage of molecular bond)

Oxidation-Reduction (electrons change = color change)

Photolysis (break of covalent bond from light exposure)

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Most common functional groups to be oxidized/reduced

Hydroxyl group (OH) next to aromatic ring

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Most common functional groups to be hydrolyzed

Ester (carbonyl to OR)

Amide (carbonyl to N)

Beta-Lactam ring

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Pharmacodynamics

What the drug does to the body; mechanism of action

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Pharmacokinetics

What the body does to the drug (absorption, distribution, metabolism, excretion)

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What drugs to separate from polyvalent cations (chelating agent)

FQs

Tetracyclines

Levothyroxine

Oral bisphosphonates

Cefixime

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Capecitabine (prodrug)

Fluorouracil (active metabolite)

- 5-FU

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Clopidogrel (prodrug)

Active metabolite

- CYP2C19 substrate

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Codeine (prodrug)

Morphine (active metabolite)

- CYP2D6 substrate

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Colistimethate (prodrug)

Colistin (active metabolite)

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Cortisone (prodrug)

Cortisol (active metabolite)

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Famciclovir (prodrug)

Penciclovir (active metabolite)

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Fosphenytoin (prodrug)

Phenytoin (active metabolite)

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Isavuconazonium sulfate (prodrug)

Isavuconazole (active metabolite)

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Levodopa (prodrug)

Dopamine (active metabolite)

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Lisdexamfetamine (prodrug)

Dextroamphetamine (active metabolite)

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Prednisone (prodrug)

Prednisolone (active metabolite)

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Primidone (prodrug)

Phenobarbital (active metabolite)

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Tramadol (prodrug)

Active metabolite

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Valacyclovir (prodrug)

Acyclovir (active metabolite)

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Valganciclovir (prodrug)

Ganciclovir (active metabolite)

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P-gp Substrates

Anticoagulants (apixaban, rivaroxaban)

Cardiovascular drugs (diltiazem, verapamil, digoxin)

Immunosuppressants (cyclosporine, tacrolimus)

HCV drugs (sofosbuvir)

Others (colchicine)

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P-gp Inducers

Carbamazepine

Phenobarbital

Phenytoin

Rifampin

St. John's Wort

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P-gp Inhibitors

Anti-infectives: (clarithromycin, itraconazole, posaconazole)

cardiovascular drugs: (amiodarone, diltiazem, verapamil)

HIV drugs (cobicistat, ritonavir)

HCV drugs (ledipasvir)

Others (cyclosporine)

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CYP-2C9 Inducers

Rifampin

St. John's Wort

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CYP-2C9 Inhibitors

Amiodarone

Azole antifungals

Metronidazole

SMX/TMP

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CYP-3A4 Substrates

Statins: lovastatin, simvastatin, atorvastatin

Opioids: fentanyl, hydrocodone, oxycodone, methadone

Immunosuppressants/Anti-rejection: tacrolimus, cyclosporine, sirolimus

CV: nifedipine, amiodarone, amlodipine, bosentan, diltiazem, verapamil, eplerenone, ivabradine, quinidine, ranolazine, tolvaptan

Anticoagulants: apixaban, rivaroxaban, R-warfarin

HIV: NNRTIs

PDE-5i: avanafil, sildenafil, tadalafil, vardenafil

Ethinyl estradiol

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CYP-1A2 Substrates

R-warfarin

Theophylline

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CYP-2C9 Substrates

S-warfarin

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CYP-2C19 Substrates

clopidogrel

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CYP-2D6 Substrates

- Analgesics (codeine, hydrocodone, meperidine, methadone, oxycodone, tramadol)

- Antipsychotics/Antidepressants

- Others (carvedilol, DM, flecainide, methamphetamine, metoprolol, propafenone, propranolol, tamoxifen)

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If on warfarin and adding on amiodarone?

Decrease warfarin dose 30-50% depending on INR

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If on digoxin and adding amiodarone?

Decrease digoxin dose by 50%

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What increases digoxin toxicity risk?

Loop diuretics

Low potassium

High calcium

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Which statins are metabolized by CYP3A4?

Simvastatin, atorvastatin, lovastatin (SAL)

- Simvastatin and lovastatin CI with strong CYP3A4i

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How does valproic acid affect lamotrigine?

Decreases lamotrigine metabolism and increases levels which can cause SJS/TENS

- use Lamictal starter kit

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Increased Serotonergic Toxicity Risk Meds

Antidepressants

MAOi

Opioids

Triptans

St. Johns wort, L-tryptophan

Buspirone

Lithium

Dextromethorphan

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Increased Hyperkalemia Risk Meds

RAAS drugs

Potassium-sparing diuretics (amiloride, triamterene)

KCl

Tacrolimus, cyclosporine

SMX/TMP

Canagliflozin

Drospirenone-containing oral contraceptives

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Increased QT Prolongation Risk Meds

Antiarrythmics (Class 1a, 1c, III)

Anti-infectives (hydroxychloroquine, azole antifungals, macrolides, quinolones)

Antidepressants (SSRIs, TCAs, mirtazapine, trazodone, venlafaxine)

1st and 2nd Gen Antipsychotics

Antiemetics (5-HT3 antagonists, droperidol, metoclopramide, promethazine)

Oncology (leuprolide, TKIs, arsenic trioxide)

Others (methadone, hydroxyzine, cilostazol, donepezil, loperamide, ranolazine, solifenacin)

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Which SSRI is the safest for patients with CVD?

Sertraline

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CBC (complete blood count)

a set of tests that include all WBC, RBC and platelet measurements.

<p>a set of tests that include all WBC, RBC and platelet measurements.</p>
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BMP (basic metabolic panel)

A group of 7-8 tests

<p>A group of 7-8 tests</p>
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Drug causes of agranulocytosis (decreased neutrophils, basophils, eosinophils)

Clozapine

PTU

Methimazole

Carbamazepine

SMX/TMP

Isoniazid

Procainamide

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Causes of increased calcium

Vitamin D

Thiazides

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Causes of decreased calcium

Long-term heparin

Loop diuretics

Bisphosphonates

Cinacalcet

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Causes of decreased magnesium

PPIs

Diuretics

Amphotericin B

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Causes of increased phosphate

CKD

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Causes of increased potassium

RAAS drugs

Potassium-sparing diuretics (amiloride, triamterene)

KCl

Tacrolimus, cyclosporine

SMX/TMP

Canagliflozin

Drospirenone-containing oral contraceptives

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Causes of decreased potassium

Beta-2 agonists

Diuretics

Insulin

Sodium Polystyrene Sulfate (SPS)

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Causes of increased sodium

Hypertonic saline

Tolvaptan

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Causes of decreased sodium

Carbamazepine

Oxcarbazepine

SSRIs

Diuretics

Desmopressin

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Causes of decreased bicarbonate

Topiramate

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Causes of increased BUN

Renal impairment and dehydration

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Causes of increased WBCs

Systemic steroids

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Causes of decreased WBCs

Clozapine

Chemotherapy

Carbamazepine

Immunosuppressants

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Causes of increased eosinophils

Asthma, inflammation, parasitic infection

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Causes of increased basophils

Hypersensitivity reaction

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Causes of increased lymphocytes

Viral infections, lymphoma

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Causes of decreased lymphocytes

Bone marrow suppression, HIV, systemic steroids

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RBC average life-span

120 days

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Causes of increased RBCs and Hgb

ESAs

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Causes of decreased RBCs

Chemotherapy

Deficiency anemia (B12, folate)

Hemolytic anemia

Sickle cell anemia

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Causes of increased MCV

B12 or folate deficiency

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Causes of decreased MCV

Iron deficiency

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Causes of decreased folic acid (folate)

Phenytoin/fosphenytoin

Phenobarbital/primidone

Methotrexate

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Causes of decreased vitamin B12

PPIs

Metformin

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Causes of decreased reticulocyte count

Untreated anemia

Bone marrow suppression

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Coombs Test, Direct

Used to diagnose immune-mediated hemolytic anemia

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Drug causes of immune-mediated hemolytic anemia

PCNs + cephalosporins

Isoniazid

Levodopa

Methyldopa

Quinidine

Quinine

Rifampin

Sulfonamides

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G6PD Test

Used to determine if hemolytic anemia is due to G6PD deficiency

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Food/Drugs that trigger RBC destruction with G6PD deficiency

Fava Beans

Dapsone

Methylene Blue

Nitrofurantoin

Pegloticase

Primaquine

Rasburicase

Quinidine

Quinine

Sulfonamides

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What does Anti-Xa monitor?

LMWH (therapeutic dose - get peak level 4h after)

UFH (get level 6h after IV infusion starts)

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What does PT/INR monitor?

Warfarin

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What can falsely and actually increase PT/INR?

Falsely: daptomycin, oritavancin, telavancin

Actually: liver disease

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What does aPTT or PTT monitor?

UFH (get level 6h after IV infusion starts)

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What can falsely increase aPTT/PTT?

Oritavancin, televancin

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Platelet lifespan and what can cause decreased platelets?

Average 7-10 days

Decreased by:

Heparin + LMWH

Fondaparinux

Linezolid

Valproic Acid

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What can cause decreased albumin?

Cirrhosis

Malnutrition

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What drugs are highly protein bound?

Warfarin

Calcium

Phenytoin