PHARM Flashcards
Cyclosporine-Tacroglimus -> Clinical Use
3
- Reduce acute transplant rejection
- Psoriasis
- Rheumatoid Arthritis
Calcineurin Inhibitors
2
- -Cyclosporine
- Tacrolimus
Cyclosporine-Mechanism
- Binds cyclophilin
- Blocks T cell activation
- Prevents IL-2 transcription
Tacrolimus-Mechanism
- Binds FK506 binding protein
- inhibition of IL-2 transcription
Binds FK506 binding protein
Tacrolimus-Mechanism
Side effects-Cyclosporine
- Nephrotoxicity
- Neurotoxicity
- Gingival hyperplasia
- Hirsutism
- Hypertension
Side effects-Tacrolimus
- ↑ risk of neurotoxicity compared to cyclosporine
- ↑ risk of diabetes
- -Nephrotoxicity
- -Hypertension
mycophenolate mofetil-MOA
inosine monophosphate dehydrogenase inhibitor->By inhibiting de novo guanosine nucleotide synthesis, T and B lymphocyte proliferation is disrupted.
mycophenolate mofetil-Side effect
Bone marrow suppression
used in patients who cannot tolerate calcineurin inhibitors due to the frequency of neurotoxicity and nephrotoxicity.
mycophenolate mofetil
sirolimus-side effect
Delayed wound healing
hepatic artery thrombosis, hyperlipidemia, and dermatologic complications.
sirolimus-MOA
blocks signal transduction at the IL-2 receptor
anti-CD3 antigen complex monoclonal antibody-Side effect
associated with viral or other infectious reactivation, such as reactivation of tuberculosis or viral hepatitis
Skin thinning is a very common side effect associated with
steroids
Amides -> Anesthetics
lidocaine, mepivacaine, prilocaine, bupivacaine, etidocaine, and ropivacaine and levobupivacaine
_tienen una i antes del -caine
Esters -> Anesthetics
chloroprocaine, procaine, and tetracaine
serotonin syndrome->
SSRIs, SNRIs, TCAs,tramadol, ondansetron, triptans, MDMA, and dextromethorphan
Aminoglycosides
Amikacin Gentamicin Neomycin Tobramycin Streptomycin
Binds to aminoacyl site of 16S rRNA (part of 30S subunit) → misreading of genetic code and inhibition of translocation
Aminoglycosides
Mechanism of Bacterial Resistance-> Inactivation of drug via acetylation, adenylation, or phosphorylation by bacterial transferase enzymes
Aminoglycosides
Adverse Effects->Aminoglycosides
Nephrotoxicity (acute tubular necrosis)
Ototoxicity (vestibular and/or cochlear damage, potentiated by loop diuretics)
Neuromuscular blockade (contraindicated in myasthenia gravis)
Teratogenic
PX with an acute cerebrovascular accident (CVA)
Tx
-Alteplase (also called tissue plasminogen activator or tPA)->increasing fibrin’s affinity for endogenous plasminogen-> increased activation of plasmin
inhibits vitamin K-dependent carboxylation of factors II, VII, IX, and X.
Warfarin
inhibit cyclooxygenase
Aspirin, ibuprofen, and naproxen
direct inhibitor of thrombin
Argatroban
propagates a patient’s endogenous antithrombin, which inhibits thrombin and activated factor X
Heparin
Medication for type II diabetes that should be avoided in patients with heart failure, due to the risk of fluid retention.
Thiazolidinediones (TZDs) -> (pioglitazone, rosiglitazone)->
Activation of peroxisome proliferator-activated receptor gamma in adipocytes
Activation of peroxisome proliferator-activated receptor gamma in adipocytes to promote adipogenesis and fatty acid uptake and increase insulin-dependent glucose uptake.
Thiazolidinediones (TZDs) -> (pioglitazone, rosiglitazone)
Contraindications->Thiazolidinediones
Heart failure Fluid overload Active liver disease Bladder cancer Type 1 diabetes Pregnancy Macular edema
Inhibition of α-glucosidases
acarbose
oral antidiabetic agent that can cause diarrhea and gastrointestinal upset.
acarbose
work via inhibition of dipeptidyl peptidase IV, which normally functions to break down incretins (such as GIP and GLP-1) responsible for increased insulin synthesis/release and decreased glucagon release
Gliptins such as sitagliptin
works primarily via inhibition of hepatic gluconeogenesis->Increase insulin sensitivity
Metformin
also contraindicated in decompensated CHF and Renal failure, this is due to an increased risk of lactic acidosis
Metformin
work via stimulation of insulin release from the pancreas
Sulfonylureas
Side effects include hypoglycemia and weight gain (DM tx)
Sulfonylureas
Stimulation of glucose-dependent insulin release
GLP-1 agonists
Liraglutide
Semaglutide
Dulaglutide
GLP-1 agonists
DPP-4 normally degrades glucagon-like peptide-1 (GLP-1)
DPP-4 inhibitors therefore prevent degradation of GLP-1
DPP-4 inhibitors
DPP-4 inhibitors
Sitagliptin
Saxagliptin
Linagliptin
SGLT-2 inhibitors
Canagliflozin
Empagliflozin
expressed in the proximal tubule and mediates reabsorption of approximately 90 percent of the filtered glucose load
SGLT-2
Sulfonylureas
Glyburide
Glipizide
Tolbutamide
Chlorpropamide
hookworm infection -> first-line therapy
inhibition of microtubule synthesis
**albendazole or mebendazole
treatment of pinworm, roundworm, and hookworm.
Depolarizing neuromuscular blockade
- modulates the GABAergic system to induce a neuromuscular blockade in the helminth
- *Pyrantel pamoate
treatment of strongyloidiasis
influx of Cl- ions leading to hyperpolarization of the helminth cell membranes.
(Ivermectin)
modulates the nitric oxide and cyclooxygenase inflammatory pathways to increase the helminth’s susceptibility to phagocytosis
Diethylcarbamazine
-> treatment of filariasis
treatment of schistosomiasis
an influx of Ca++ ions, leading to muscle spasm and paralysis of the helminth
->Praziquantel
Cardiac Glycoside
1
(Digoxin)
Adverse Effects-> Digoxin
AV block Arrhythmias Blurry yellow vision Cholinergic: Diarrhea,Nausea,Vomiting Hyperkalemia
Atrial fibrillation->Decreases conduction at AV node
Heart failure-> Increases contractility
> Digoxin
Direct inhibition of Na+/K+ ATPase Indirect inhibition of Na+/Ca2+ exchanger ↑ Ca2+ concentration Increases Inotropy Stimulates Vagus nerve ↓ Heart rate
Digoxin
Risk Factors for toxicity
-> Drugs that displace Digoxin from tissue-binding sites
(3)
- > Amiodarone
- > Quinidine
- > Verapamil
Risk Factors for toxicity->digoxin
Hypokalemia
Renal failure (digoxina se extreta por el rinon)
↓ Excretion
Digoxin toxicity is characterized by electrocardiogram changes including
increased PR interval
decreased QT interval
scooping of the ST segment
T-wave inversion
selectively blocking the binding of angiotensin II to AT1 receptors
Losartan
alpha-1 receptor blocker and works by selectively blocking the alpha-1 receptors
Prazosin
Prazosin ->Uses
benign prostate hyperplasia, PTSD, and hypertension treatment
Prazosin-> secondary effects
Side effects include 1st dose orthostatic hypotension, dizziness, and headaches.
β-blocker that decreases SA and AV nodal activity by decreasing cAMP and Ca2+ currents
Metoprolol
Metoprolol-> side effects
impotence, exacerbation of COPD and asthma, bradycardia, and masking of hypoglycemia.
vasodilation of vascular smooth muscles with increased cGMP
Nitroglycerin
Nitroglycerin-> Side effects
reflex tachycardia, hypotension, flushing, and headaches
angiotensin-converting enzyme inhibitor and works by inhibiting ACE and decreasing ATII
Lisinopril
Side effects ->Lisinopril
angioedema, cough, hyperkalemia, and hypotension
Inhibit calcium ion channel
Calcium channel blockers
Antianginal therapy-> β-blockers + Nitrates
Blood Pressure ↓
Myocardial O2 consumption ↓↓
Antianginal therapy-> Nitrates
Blood Pressure↓ Contractility ↑ Ejection time↓ End-Diastolic volume↓ Heart rate↑ Myocardial O2 consumption↓
Antianginal therapy-> β-blockers
Blood Pressure↓ Contractility ↓ Ejection time↑ End-Diastolic volume - Heart rate↓ Myocardial O2 consumption↓
Tx for a flare of her Crohn’s disease in pregnant
Antibodies against tumor necrosis factor (TNF) α -> infliximab
increased risk using infliximab
tuberculosis reactivation, patients should get a purified protein derivative (PPD) test
purine analogue and inhibits purine nucleotide synthesis and metabolism
6-mercaptopurine
inhibits dihydrofolate reductase. It also inhibits purine synthesis and decreases the production of inflammatory cytokines
Methotrexate (MTX)
Tx elevated intracranial pressure (ICP) ICP ≥ 20 mm
mannitol -> causes osmotic diuresis and increased urine output
** may cause (or worsen) pulmonary edema (due to rapid increase i the vascular hydrostatic pressure)
Tx for SIADH
Demeclocycline is an ADH antagonist
Tx for DI
Desmopressin is a synthetic version of ADH and can be used to treat central diabetes insipidus (DI).
first-line therapy for patients that present with decompensated heart failure
Furosemide -> loop diuretic
should not be used in cases of elevated ICP
Glucocorticoids->unless the elevation is due to malignancy
Contraindications Mannitol
- Anuria
- Heart failure
Contraindications -> Spironolactone
- Addison disease (chronic adrenal insufficiency)
- Hyperkalemia
Contraindications -> Thiazide diuretics
Gout (thiazides reduce the clearance of uric acid since they compete for the same transporter)
Hypokalemia
Hypotension
Sulfa allergy
Contraindications ->Loop diuretics
Hyperuricemia Sulfa allergies (ethacrynic acid is the only loop diuretic that can be used in a patient with a sulfa allergy)
Contraindications >Acetazolamide
Sulfa allergy
Nephrolithiasis (acetazolamide promotes calcium phosphate stone formation)
chronic graft-versus-host disease (GVHD)
Skin is the most commonly affected organ in chronic GVHD, and skin findings are usually classified as lichen planus-like or sclerotic.
prophylactic agent for the prevention of chronic GVHD
methotrexate + leucovorin
*Administering leucovorin (folinic acid) along with methotrexate can reduce the likelihood and severity of methotrexate adverse effects