pharmacology

testing all aspect of pharmacology

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

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