Studied by 30 people
Name the drug used for disorders of balance and spatial orientation( motion sickness)
scopolamine
It is a drug used to treat nausea and vomiting during travel as well as treatment in post operation and opioid analgesic . It acts through competitive inhibition of muscarinic receptors
RENAL/URINE
which drug cause these side effects?
sulfonamide hypersensitivity
hypokalemia and alkalosis
hypocalcemia, hypomagnesemia
hyperuricemia, ototoxicity.
furosemide
along with torsemide, and ethacrynic acid
Mechanism: Na+/K+/2Cl− transporter inhibition, results in:
– ↓ intracellular K+ in TAL
– ↓ back diffusion of K+
– ↓ positive potential
– ↓ reabsorption of Ca2+ and Mg2+
– ↑ diuresis •
Uses: – Acute pulmonary edema – Heart failure – Hypertension – Refractory edemas – Hypercalcemic states (limited use
Drug interactions – Aminoglycosides (enhanced ototoxicity) – Lithium (chronic loop administration, ↓ clearance) – Digoxin (↑ toxicity due to electrolyte disturbances)
which drug utilize these Mechanisms?
: Na+/K+/2Cl− transporter inhibition, results in:
– ↓ intracellular K+ in TAL
– ↓ back diffusion of K+
– ↓ positive potential
– ↓ reabsorption of Ca2+ and Mg2+
– ↑ diuresis •
furosemide
along with torsemide, and ethacrynic acid
Which drug Results in
↑ intracellular Na+
– Decreases Na+/Ca2+ exchange
– Increases intracellular Ca2+
– Increases Ca2+ release from sarcoplasmic reticulum
– Increases actin-myosin interaction – Increases contractile force
digoxin
this is a direct effect
Indirect effect: inhibition of neuronal Na+-K+ ATPase (results in ↑ vagal activity
this is the pharmacokinetics of which drug
caution in renal impairment ,need loading dose (LD) –,Tissue protein binding (large Vd): displacement by other drugs (verapamil, quinidine)
digoxin
also used for : CHF; supraventricular tachycardias, except Wolff-Parkinson-
White syndrome
which drug cause these Side effects and what is the management ?
Early signs include anorexia, nausea, ECG changes –,Later signs include disorientation, visual effects (yellow-green color disturbances, blurry vision) and In toxic doses, any cardiac arrhythmias.
digoxin
Management of toxicity: use of Fab antibodies toward digoxin; supportive therapy (electrolytes and antiarrhythmics class IB)
what are the side effects of enalapril?
Enalapril is a prodrug of an ACE inhibitor used to treat hypertension and congestive heart failure.
Most common adverse effects of enalapril include cough, hypotension, stupor, headache, dizziness and fatigue.
activated charcoal can be used within 1-2hrs
what is the adverse effect of hydrochlorothiazide?
Side effects: – Sulfonamide hypersensitivity – Hypokalemia and alkalosis – Hypercalcemia – Hyperuricemia (actively secreted by the OAT) – Hyperglycemia – Hyperlipidemia (except indapamide)
what is the MECH of Hydrochlorothiazide?
Mechanism: Na+/Cl− transporter inhibition,
results in: – ↑ luminal Na+ and Cl− in DCT
– ↑ diuresis
which drug is useful in treatment of
Hypertension,
CHF – Nephrolithiasis (calcium stones)
– Nephrogenic diabetes insipidus
hydrochlorothiazide
Drug interactions and cautions: – Digoxin (↑ toxicity due to electrolyte disturbances
side effects of hydrochlorothiazide on the heart.
seizures, decreased urine, drowsiness, dry mouth, excessive thirst, increased heart rate or pulse, muscle pains or cramps, nausea or vomiting, or unusual tiredness or weakness. These may be symptoms of a condition called hypokalemia or potassium loss.
this drug usually aids IN decrease preload
adverse effect of aminoglycosides
nephrotoxity -tubular damage
organophosphate poisoning symptoms and treatment.
Symptoms include increased saliva and tear production, diarrhea, nausea, vomiting, small pupils, sweating, muscle tremors, and confusion.
atropine, pralidoxime (2-PAM), and benzodiazepines
which part of the brain is responsible for motion sickness?
cerebellum and brainstem
drugs that trigger fluid volume and electrolyte disorders to cause hypokalemia
Drugs: acetazolamide and dorzolamide
carbonic anhydrase inhibitor
furosemide, torsemide, and ethacrynic acid .these are loop diruetic on TAL
Diuretics that block Na+ reabsorption at segments above the collecting ducts will increase sodium load to the collecting tubules and ducts (“downstream”). This results in increased loss of K+ → hypokalemia.
what is the mechanisms of drug interactions of heparin-aspirin?
it can cause pt to bleed out intra cranial hemorrhage
Heparin catalyzes the binding of antithrombin III (a serine protease inhibitor) to factors IIa, IXa, Xa, XIa, and XIIa, resulting in their rapid inactivation
Aspirin – Irreversibly inhibits COX in platelets →↓ activation – Low doses prevent MI and recurrence; prophylaxis in atrial arrhythmias and TIAs – Adverse effects (see Section VI, Drugs for Inflammatory and Related Disorders
adverse effect of isoniazid in HIV infection
Hepatitis (age-dependent) •
Peripheral neuritis (use vitamin B6)
• Sideroblastic anemia (use vitamin B6)
• SLE in slow acetylators (rare)
why low doses of aspirin prevent thromboemboli better than acetaminophen
answer
aspirin binds to cox1 enzyme blocking archononic acid which puts a break on PGh2 which makes it harder for blood to cloth. aspirin is bound to cox 1 permently so the body takes time to produce more
adverse effects of drugs on the ear
adverse effect, gentamicin; ototoxicity
drugs used to treat BPH
Alpha-1 Blockers • Decrease arteriolar and venous resistance • Reflex tachycardia • Drugs: prazosin, doxazosin, terazosin • Uses: – Hypertension – BPH: relax the smooth muscle of the prostate and bladder neck, which allows urine to flow more easily • Side effects: “first-dose” syncope; orthostatic hypotension; urinary incontinence • Advantage: good effect on lipid profile (↑ HDL, ↓ LDL)
Antibacterial resistant to beta-lactamases
Aztreonam • Mechanism of action: – Same as for penicillins and cephalosporins – Resistant to beta-lactamases • Uses: – IV drug mainly active versus gram-negative rods – No cross-allergenicity with penicillins or cephalosporins
Antibacterial resistant to beta-lactamases
Imipenem and Meropenem
• Spectrum: – Gram-positive cocci, gram-negative rods (e.g., Enterobacter, Pseudomonas spp.), and anaerobes
– Important in-hospital agents for empiric use in severe life-threatening infections
• Pharmacokinetics: – Imipenem is given with cilastatin, a renal dehydropeptidase inhibitor, which inhibits imipenem’s metabolism to a nephrotoxic metabolite
– Both drugs undergo renal elimination— ↓ dose in renal dysfunction
• Side effects: – GI distress – Drug fever (partial cross-allergenicity with penicillins) – CNS effects, including seizures with imipenem in overdose or renal dysfunction
Comparison of heparin and enoxaparin in subjects in experiment
Heparin is a mixture of sulfated polysaccharides with molecular weights of 15–20,000 daltons. Low-molecular-weight (LMW) heparins (e.g., enoxaparin) have a potential advantage of longer half-life, less thrombocytopenia, and possible enhanced activity against factor Xa.
Adverse effect of acetaminophen
nausea and vomiting
N-acetylcysteine treatment
adverse effect of furosemide;
hearing loss-ototoxicity
adverse effects of drugs
withdrawal of clonidine cause hypertensive crisis
Alpha-2 Agonists
• Drugs: clonidine and methyldopa (prodrug) • α2 stimulation: ↓ in sympathetic outflow; ↓ TPR but also ↓ HR
• Uses: – Mild-to-moderate hypertension (both) – Opiate withdrawal (clonidine) – Hypertensive management in pregnancy (methyldopa)
• Side effects: positive Coombs test (methyldopa); CNS depression (both); edema (both)
• Drug interactions: tricyclic antidepressants ↓ antihypertensive effects of α2 agonist
adverse effect of phenylephrine
α1 Agonists Systemically, alpha-1 agonists increase mean BP via vasoconstriction.
• Increased BP may elicit a reflex bradycardia
• Cardiac output may be ↓ but also offset by ↑ venous return • Drugs and uses: – Phenylephrine: nasal decongestant and ophthalmologic use (mydriasis without cycloplegia), hypotensive states
acromegaly treatment
Somatostatin(Octreotide)
treats
Acromegaly, carcinoid and secretory-GI tumors
diazepam overdose
coma
acts on (GABA), an inhibitory neurotransmitter in the central nervous system. Potentiation of GABA interaction with GABAA receptors involves BZ1 and BZ2 binding sites
treatment
Sedation, anterograde amnesia; in severe OD (or IV use), reverse with flumazenil
Rebound insomnia, rebound anxiety caused by withdrawl
disorders of the esophagus
Drugs that decrease gastric acid secr eation by inhibit H+-K+ ATPase
Esomeprazole magnesium (Nexium)
Inhibits gastric acid secretion by inhibiting H+-K+-ATPase enzyme system at secretory surface of gastric parietal cells.
neoplasm drug treatment for mestatic prostate cancer
Enzalutamide. Enzalutamide is a nonsteroidal AR inhibitor that is approved to treat metastatic and non-metastatic castration-resistant prostate cancer as well as metastatic castration-sensitive prostate cancer.
\n Enzalutamide is a competitive androgen receptor (AR) inhibitor that has a threefold inhibition on the androgen signaling pathway without significant AR agonist activity
name of Gastroparesis diabetes medication
Metoclopramide,
the only FDA-approved medication for gastroparesis, is considered a first-line agent in the treatment of diabetic gastroparesis. Metoclopramide is a dopamine2 (D2)-receptor antagonist, 5-HT4 (serotonin)-receptor agonist, and 5-HT3-receptor antagonist that stimulates smooth muscle contraction.
side effects of valproic acid
valproic acid –
Mechanism: º Blocks axonal Na+ channels in their inactivated state, But also inhibition of GABA transaminase , Blockade of T-type Ca2+ channels
– Uses: º Seizure states º,Mania of bipolar disorders º Migraine prophylaxis
– Pharmacokinetics: inhibits cytochrome P450s
– Side effects: º Hepatotoxicity (from toxic metabolite) º Thrombocytopenia , Pancreatitis , Alopecia
– Teratogenicity: spina bifida
drug treatment :Oral carnitine
adverse effect of isotretinoin
alopecia
finasteride and minoxidil, are used in the treatment of male-pattern baldness. Minoxidil is currently the only medicine available to treat female-pattern baldness. Finasteride is available as oral tablets which are only used for men.
adverse effects of piroxicam
gi inflammation -gastritis
Misoprostol
Piroxicam is in a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). Piroxicam works by reducing hormones that cause inflammation and pain in the body. Piroxicam is used to reduce the pain, inflammation, and stiffness caused by rheumatoid arthritis and osteoarthritis.
The anti inflammatory effect of Piroxicam may result from the reversible inhibition of cyclooxygenase, causing the peripheral inhibition of prostaglandin synthesis.
treatment for migraine
•Ergot derivatives- (5-HT1D)- Ergotamine.
•Triptans- (5-HT1D/1B) agonists-
adverse effect of midazolam
respiratory depression
it is a benzo
Potentiation of GABA interaction with GABAA receptors involves BZ1 and BZ2 binding sites
Light to moderate CNS depression
Sedation, anterograde amnesia; in severe OD (or IV use), reverse with flumazenil
Single-dose or multi-dose activated charcoal, hemodialysis, or whole bowel irrigation play no role in managing benzodiazepine toxicity.
Lorazepam is a short-acting benzodiazepine commonly used to treat panic disorders, severe anxiety, and seizures
\n The effect of lorazepam in GABA-A receptors produces an increase in the frequency of opening of the chloride ion channel.
exhaustion, sedation, lethargy, addiction side effcts
why red red wine should not be used with MAO inhibitor
it causes hypertension(hypertensive crisis
cheese and wine contain the amino acid tyramine that
causes the release of norepinephrine, which acts at the alpha receptors to cause vasoconstriction. Normally, monoamine oxidase in the liver will break down tyramine rapidly. MAOIs will have an elevated blood concentration of tyramine since the amino acid will not be broken down. this cause an increased constriction of blood vessels.
what is hypertensive crisis and symptoms
In addition to high blood pressure, other physical symptoms of a hypertensive crisis include headache and shortness of breath. Mental symptoms of hypertensive crisis include confusion and seizure, all of which may be very dangerous.
treatment: Phentolamine and tolazoline
what are MAOI drugs
Isocarboxazid (Marplan)
Phenelzine (Nardil)
Selegiline (Emsam)
Tranylcypromine (Parnate)
Adverse effect of corticosteroid
candidiasis
The infection occurs because the steroids in the inhaler weaken the immune system in the mouth and throat. Oral thrush can cause discomfort and trouble eating. However, it usually can be treated quickly with antifungal medications.
Polyenes, fluoropyrimidines, echinocandins, and azoles are used as commercial antifungal agents to treat candidiasis.
disorders of hair and hair follicles alopecia treatment
Two medicines, namely finasteride and minoxidil, are used in the treatment of male-pattern baldness. Minoxidil is currently the only medicine available to treat female-pattern baldness. Finasteride is available as oral tablets which are only used for men.
Finasteride is an antiandrogenic compound that is used for the treatment of symptomatic benign prostatic hyperplasia (BPH) and male pattern hair loss in adult males by inhibiting Type II 5-alpha reductase.
Minoxidil is thought to promote the survival of human dermal papillary cells (DPCs) or hair cells by activating both extracellular signal-regulated kinase (ERK) and Akt and by preventing cell death by increasing the ratio of BCl-2/Bax.
Minoxidil is an orally effective direct acting peripheral vasodilator that reduces elevated systolic and diastolic blood pressure by decreasing peripheral vascular resistance. Minoxidil is also used topically to treat androgenetic alopecia.
Drugs Used for Treatment of Asthma
β2 agonists: albuterol, terbutaline exercise induce
• M-blocker: ipratropium, tiotropium acute asthma in copd
• Methylxanthine: theophylline inhibit PDE dec CAMP,adjunct
• Mast-cell stabilizer: cromolyn dec bronchial sensivity in response to allergen
• Steroids: flunisolide
• LT modifiers: montelukast, zafirlukast, zileuton = antigen, exercise, or drug-induced profloax used
drugs that treat erectile dysfunction
Sildenafil (Viagra), vardenafil (Levitra, Staxyn), tadalafil (Cialis) and avanafil (Stendra) are oral medications that reverse erectile dysfunction by enhancing the effects of nitric oxide, a natural chemical your body produces that relaxes muscles in the penis.
how does Sildenafil work
Sildenafil is a phosphodiesterase inhibitor used for the treatment of erectile dysfunction. In eliciting its mechanism of action, sildenafil ultimately prevents or minimizes the breakdown of cyclic guanosine monophosphate (cGMP) by inhibiting cGMP specific phosphodiesterase type 5 (PDE5)
osteitis deformans caused by Paget disease drug treatment
Bisphosphonates: Alendronate and Other Dronates
• Mechanisms: are analogs of pyrophosphate
– Directly inhibit bone resorption by inhibiting the enzyme farnesyl pyrophosphate (FPP) synthase in the mevalonate pathway (cholesterol biosynthetic pathway)
– Inhibition of FPP synthase disrupts protein prenylation, which creates cytoskeletal abnormalities in the osteoclast, promotes detachment of the osteoclast from the bone perimeter, and leads to reduced bone resorption
• Clinical uses: – Considered first-line therapy for the management of osteoporosis – Beneficial in Paget disease
– Side effects: bone mineralization defects (etidronate and pamidronate); gastrointestinal distress including esophageal ulcers (alendronate)
hyperprolactinemia treatment
Hyperprolactinemia means you have higher-than-normal levels of prolactin in your blood. The most common cause is a prolactinoma, a benign (noncancerous) tumor in your pituitary gland.
Medical treatment of hyperprolactinemia is based upon use of dopamine agonists (DA): bromocriptine, lisuride, quinagolide and cabergoline. In over 80% of cases, these drugs induce normal prolactinemia and ovulatory cycles.
PIH (DA) Cabergoline Hyperprolactinemia txt
peptic ulcer drug treatment
disorders of the stomach
Proton Pump Inhibitors • Mechanism of action: – Omeprazole and related “–prazoles” are irreversible, direct inhibitors of the proton pump (K+/H+ antiport) in the gastric parietal cell • Uses: – More effective than H2 blockers in peptic ulcer disease (PUD) – Also effective in GERD and Zollinger-Ellison syndrome – Eradication regimen for H. pylor
adverse effect, ibuprofen
gastric ulcer
Peptic ulcer disease is a well-recognised complication of NSAID use. Inhibition of COX-1 in the gastrointestinal tract leads to a reduction of prostaglandin secretion and its cytoprotective effects in gastric mucosa. This therefore increases the susceptibility to mucosal injury.
treatment
Misoprostol • Mechanism of action: PGE1 analog, which is cytoprotective →↑ mucus and bicarbonate secretion and ↓ HCl secretion • Uses: Previously for NSAID-induced ulcers, but PPIs are now use
drug treatment for hyperthyroidism
Drugs for Hyperthyroidism
• Thioamides: propylthiouracil and methimazole
– Use: uncomplicated hyperthyroid conditions; slow in onset – High-dose propylthiouracil inhibits 5′ deiodinase
– Common maculopapular rash; agranulocytosis, liver failure (PTU)
– Both drugs cross the placental barrier, but propylthiouracil is safer in pregnancy because it is extensively protein bound • Iodide
– Potassium iodide plus iodine (Lugol solution) possible use in thyrotoxicosis: used preoperatively →↓ gland size, fragility, and vascularity
– No long-term use because thyroid gland “escapes” from effects after 10 to 14 days
• I 131: most commonly used drug for hyperthyroidism
treatment for adrenal disorders that cause delayed puberty
Androgens include methyltestosterone and 17-alkyl derivatives with increased anabolic actions, e.g., oxandrolone, nandrolone.
• Uses: – Male hypogonadism and for anabolic actions →↑ muscle mass, ↑ RBCs, ↓ nitrogen excretion
– Illicit use in athletics
• Side effects: excessive masculinization, premature closure of epiphysis, cholestatic jaundice, aggression, dependenc
levothyroxine , how does it cause osteoporosis
Thyroid hormone affects the rate of bone replacement. Too much thyroid hormone (i.e. thyroxine) in your body speeds the rate at which bone is lost. If this happens too fast the osteoblasts may not be able to replace the bone loss quickly enough.
Levothyroxine is a synthetic T4 hormone used to treat hypothyroidism that can be used along with surgery and radioiodine therapy to manage thyrotropin-dependent well-differentiated thyroid cancer.
pamidronate treatment in peads pt
what is the Molecular target of lidocaine used as anesthetic
Lidocaine is an antiarrhythmic medication of the class Ib type. This means it works by blocking sodium channels and thus decreasing the rate of contractions of the heart.
it acts on voltage gate sodium potassium channel
prostate cancer treatment
.Antagonists
• Flutamide: androgen receptor blocker: used for androgen-receptor– positive prostate cancer
• Leuprolide: GnRH analog: repository form used for androgenreceptor–positive prostate cancer
what is Raloxifene used for?
Selective Estrogen-Receptor Modulators (SERMs)
Raloxifene – E-receptor agonist (bone), antagonist breast and uterus
– When used in menopause, there is no increased cancer risk
– Use: prophylaxis of postmenopausal osteoporosis, breast cancer
how to treat osteoporosis caused by prednisone?
orticosteroids tend to both reduce the body's ability to absorb calcium and increase how fast bone is broken down. The more of these drugs you take and the longer you take them, the greater your risk of developing osteoporosis.
The first choice for prevention of corticosteroid osteoporosis is a potent oral bisphosphonate—for example, alendronate or risedronate. Intravenous bisphosphonates should be considered for patients intolerant of the oral route.
\n
MOA of bisphosphonates
Bisphosphonates: Alendronate and Other Dronates
• Mechanisms: are analogs of pyrophosphate
– Directly inhibit bone resorption by inhibiting the enzyme farnesyl pyrophosphate (FPP) synthase in the mevalonate pathway (cholesterol biosynthetic pathway)
– Inhibition of FPP synthase disrupts protein prenylation, which creates cytoskeletal abnormalities in the osteoclast, promotes detachment of the osteoclast from the bone perimeter, and leads to reduced bone resorption
drugs that treat bone mineral disorders
Teriparatide
• Mechanism: recombinant DNA PTH analog
• Clinical use: 1x daily to stimulate osteoblasts and new bone formation
• Continuous infusion would stimulate osteoclast activity
• Recommended use for <2 years; may increase risk of osteosarcoma
Denosumab
• Inhibits RANK ligand, a protein which acts as the primary signal for bone removal
neuroleptic malignant syndrome treatment
Medications prescribed as treatment may include skeletal muscle relaxants, such as dantrolene; stimulators of dopamine production and activity, such as bromocriptine; and/or continuous perfusion of central nervous system depressants, such as diazepam
what is neuroleptic malignant syndrome
acne vulgaris TXT
First-line treatment for severe acne vulgaris includes an oral antibiotic, benzoyl peroxide, and a topical antibiotic (erythromycin or clarithromycin), topical retinoid, or both.
Oral isotretinoin can also be considered as a first-line option.
what are drug induced acne?
corticosteroids, lithium, anticonvulsants, barbiturates, androgenic steroids, DHEA, and medications that contain bromides or iodides,
adverse effect, narcotic analgesic
opioid pharmacological actions and include nausea, vomiting, constipation, pruritus, dizziness, dry mouth and sedation
supportive, IV naloxone txt
MOA of Prednisone
Mechanisms of action: – Cellular effects º ↓ leukocyte migration º ↑ lysosomal membrane stability →↓ phagocytosis º ↓ capillary permeability
– Biochemical actions º Inhibit PLA2 (via lipocortin expression) →↓ PGs and ↓ LTs º ↓ expression of COX 2 º ↓ platelet-activating factor º ↓ interleukins (e.g., IL-2) •
Uses: antiinflammatory and immunosuppressive
Prednisone Side effects
Side effects: – Suppression of ACTH: cortical atrophy, malaise, myalgia, arthralgia, and fever; may result in a shock state with abrupt withdrawal
– Iatrogenic cushingoid syndrome → fat deposition, muscle weakness/ atrophy, bruising, acne
– Hyperglycemia due to ↑ gluconeogenesis → increased insulin demand and other adverse effects
– Osteoporosis: vertebral fractures; aseptic hip necrosis
– ↑ gastrointestinal acid and pepsin release → ulcers, gastrointestinal bleeding
– Electrolyte imbalance: Na+/water retention → edema and hypertension, hypokalemic alkalosis, hypocalcemia
– ↓ skeletal growth in children
– ↓ wound healing, ↑ infections (e.g., thrush)
– ↑ glaucoma, ↑ cataracts (via ↑ sorbitol)
– ↑ mental dysfunction
Cyclophosphamide
MOA -Alkylating agent— attacks guanine N7
TXT —dysfunctional DNA Non-Hodgkin, ovarian, breast cancer, neuroblastoma
SIDE EFFECTS -BMS, hemorrhagic cystitis (mesna, traps acrolein and is protective),alopecia
Note 
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