Drugs central Flashcards by Kjirsten Carlson

Q

What drug can treat river blindness (onchocerca volvulus) and what is its action?

A

Ivermectin

- activated GABA receptors thereby leading to worm paralysis and death

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Q

What is the MOA of praziquantel and what is its clinical use?

A

MOA: Increases cell Ca uptake, causing parasite contraction and paralysis
Use: schistosomiasis and neurocysticercosis

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Q

Bitolterol

A

beta 2 agonist

used for asthma and t treat hyperkalemia at high doses

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Q

Pirbuterol

A

beta 2 agonist

used for asthma and to treat hyperkalemia at high doses

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Q

Terbutaline

A

Beta 2 agonist- used to reduce uterine contractions during preterm labor
- and to treat bronchospasm during status epilepticus

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Q

Ritodrine

A

Beta2 agonist used to reduce uterine contractions during preterm labor

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Q

Side effects of Penicillin?

A

coombs positive hemolytic anemia, allergic reaction

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Q

What penicillin should you not give to people with mono?

A

Ampicillin

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Q

What is the clinical use of Ampicillin?

A

HELPS kill Enterococci:
H influenzae
E coli
Listeria
Proteus
Salmonella
also gram positive and negative cocci

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Q

Fluoxetine

A

SSRI

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Paroxetine

A

SSRI

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Q

Sertraline

A

SSRI

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Fluvoxamine

A

SSRI

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Q

Escitalopram

A

SSRI

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Q

Citalopram

A

SSRI

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Q

What drugs can cause serotonin syndrome if given together?

A

SSRI and MAO inhibitors:

changes in mental status, hyperthermia, muscle stiffness, myoclonus

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Q

What are the first generation TCAs?

A

Desipramine
Nortriptyline
Imipramine
Amitriptyline
Doxepin

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Q

Desipramine

A

TCA

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Nortriptyline

A

TCA

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Imipramine

A

TCA

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Amitriptyline

A

TCA

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Doxepin

A

TCA

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Q

Amoxapine

A

TCA- 2nd gen

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Q

Trazodone

A

TCA- 2nd gen

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Bupropion

TCA- 2nd gen

What are the 2nd generation TCAs?

1. Amoxapine 2. Trazoddone 3. Bupropion

MOA of the TCAs

Block the reuptake of NE and serotonin | - also have anti muscarinic, histamine, and alpha adrenergic receptors

What drug can you give for fibromyalgias?

TCAs

What TCA is used to treat neuropathic pain?

Amitriptyline

TCAs can cause seizures when given with which drug class?

MAO inhibitors

Nefazodone

Heterocyclic antidepressant, blocks the reuptake of NE and Serotonin

Venlafaxine

Heterocyclic antidepressant, blocks the reuptake of NE and Serotonin

Maprotiline

Heterocyclic antidepressant, blocks the reuptake of NE and Serotonin

Mirtazapine

heterocyclic antidepressant - inhibits activation at alpha2 adrenergic receptors and at 5HT2 receptors, thereby increasing the release of NE and serotonin

Which antidepressant should you give to a depressed anorexic pt?

Mirtazapine- causes increased appetite and weight gain | - if she has atypical depression: MAO inhibitor

Tranylcypromine

MAO inhibitor

Phenelzine

MAO inhibitor

Isocarboxazid

MAO inhibitor

MOA of MAO inhibitors?

- MAO A causes serotonin and NE metabolism - MAO B causes DA metabolism - thus the levels of serotonin, DA, and NE increase

Clinical use of MAO inhibitors?

atypical depression, specific phobias, panic disorder

Selegiline

- selectively inhibits MAO B thereby resulting in increased levels of DA - used in the tx of PD

How can MAO inhibitors cause hypertensive crisis?

- MAO is also responsible for metabolizing tyramine in wine and cheese - if ppl cant degrade tyramine, it stimulates the release of Epi and NE leading to a hypertensive crisis

Lithium: MOA and clinical use

- inhibits the phosphoinositol second messenger system | Use: bipolar disorder, SIADH, schizoaffective disorder

Toxicities of Lithium? (4)

1. Fine hand tremor 2. Hypothyroidism 3. Nephrogenic diabetes insipidus 4. Leukoctosis

What two drugs can cause nephrogenic diabetes insipidus?

1. Lithium | 2. Demeclocyline

Haloperidol

antipsychotic- typical, blocks postsynaptic DA2 receptors

Chlorpromazine

antipsychotic- typical, blocks postsynaptic DA2 receptors

Thioridazine

antipsychotic- typical, blocks postsynaptic DA2 receptors

Fluphenazine

antipsychotic- typical, blocks postsynaptic DA2 receptors

Side effects of the typical antipsychotic agents?

Sedation - anticholinergic side effects - Extrapyramidal side effects - galactorrhea and amenorrhea due to elevated level of prolatin

What are the EPSEs assoc with the typical antipsychotics?

1. Acute dystonia: muscle spasms 2. Akinesia: loss of voluntary movement 3. Akathisia: motor restlessness 4. Tardive dyskinesia: involuntary oral-facial movements

How do you treat neuroleptic malignant syndrome?

Dantrolene (muscle relaxant) and DA agonists

Clozapine

Atypical antipsychotic: block both 5HT2 and dopamine receptors

Risperidone

Atypical antipsychotic: block both 5HT2 and dopamine receptors

Olanzapine

Atypical antipsychotic: block both 5HT2 and dopamine receptors

Ziprasidone

Atypical antipsychotic: block both 5HT2 and dopamine receptors

Aripriprazole

Atypical antipsychotic: block both 5HT2 and dopamine receptors

Quetiapine

Atypical antipsychotic: block both 5HT2 and dopamine receptors

Side effects of the atypical antipsychotic agents?

- mild wright gain - parkinsonism symptoms - Clozapine can cause mild leukopenia and agranulocytosis

What drugs can cause agranulocytosis?

1. Clozapine 2. Carbamazepine 3. Colchicine 4. PTU 5. Methimazole 6. Dapsone

What are the short acting Benzos?

- triazolam | - midazolam

What are the long acting benzos?

- diazepam - prazepam - clonazepam - flurazepam

Clinical uses of benzos?

1. Anxiety 2. Seizures 3. Status epilepticus 4. Alcohol withdrawal

Which two benzos are also used as anesthetics?

Midazolam and diasepam

How do you treat overdose of BZDs?

Flumazenil

Which benzos should you avoid in the elderly?

- the long acting due to an increased risk of sedation and ataxia

Thiopental

Barbiturate | - can be used for the induction of anesthesia

Treatment of neonatal hyperbilirubinemia

Phenobarbital

What patient populations shoudl you avoid Barbs in?

- liver disease - pregnancy - porphyria - alcohol/benzo/CNS depressant use

Phenytoin: MOA

decreases the flow of Na and Ca ions across the cell membrane

What drug is used to treat trigeminal neuralgia?

Phenytoin

What drug is used to treat torsades de pointes?

Phenytoin

Toxicities of phenytoin?

1. Nystagmus 2. Gingival hyperplasia 3. Drug induced lupus 4. Fetal hydantoin syndrome

What is Fetal hydantoin syndrome and what drug causes it?

Phenytoin: fetal growth deficiency, congenital cardiac and palate malformations

What is the only seizure drug that causes lymphadenopathy?

Phenytoin

Lamotrigine

Antiepileptic that acts by inhibiting sodium channels and inhibits the release of glutamate from nervous tissue

What drug is used in the prevention of migraines?

Valproic acid

Toxicities of Vaproic acid?

Hepatotoxicity - thrombocytopenia - teratogen: neural tube defects

MOA of valproic acid?

- increase Na channel inactivation and increases GABA concentration

What are the first line agents for tonic clonic seizures?

1. Phenytoin 2. Carbamazepine 3. Valproic acid

What is the first line treatment of simple partial and simple complex seizures?

Carbamazepine

First line treatment for Absence seizures?

Ethosuximide

First line treatment for status epilepticus: prophyalxis versus acute

Prophylaxis: phenytoin Acute: Benzodiazepines

MOA of ethosuximide?

blocks thalamic T type Ca channels

Oxcarbazepine

antiepileptic- in same class as carbamazepine

Carbamazepine: MOA

- inhibits the flow of Na ions through Na channels

Toxicities of Carbamazepine?

- hepatotoxicitiy - agranulocytosis - aplastic anemia

Tiagibine

inhibits the reuptake of GABA in the synaptic cleft | - used for partial seizures

Vigabatrin

antiepileptic that acts by inhibiting the breakdown of GABA via inhibition of GABA transaminase

What are the two phases of succinylcholine NMJ blockade?

- Phase I: results in continuous depolarization at the NMJ resulting in muscle fasciculations, no antidote and cholinesterase inhibitors will only potentiate the block - Phase II: the receptor is then desensitized and will no longer transmit an action potetion- can be reversed with a cholinesterase inhibitor

Succinylcholine + ? = Malignant hyperthermia, tx?

Halothane! | tx: dantrolene

Pancuronium (and all of the curoniums)

- copmetatvely binds to nicotinic receptors at the NMJ

How can you reverse the effects of pancuronium?

neostigmine

Which local anesthetics are the esters and which ones are the amides?

Esters: procaine, cocaine, teracaine, benzocaine Amides: bupivacaine and lidocaine (have two i's in them) - esters tend to have a shorter duration of action than amides

MOA of local anesthetics?

Block the Na channels on neuronal cell membranes

What are usually given with local anesthetics?

- vasoconstrictors like epinephrine

Halothane + fluranes = MOA?

- not sure, maybe directly activate GABAa receptors throughout the brain thereby leading to decreased neuronal activity

Propofol

General IV anesthetic | - causes chemical pancreatitis

Etomidate

General IV anesthetic | - acts to prolong the activity at teh GABAa receptor

which IV anesthetic agent can cause adrenal suppression?

Etomidate

Ketamine

- IV anesthetic | - acts as an NMDA receptor antagonist decreasing neuronal cell conduction

Which IV anesthetic agent can cause hallucinations?

Ketamine

which antiepileptic can cause a rare but fatal hepatotoxicity?

valproic acid

Which epilepsy drugs can cause SJS?

1. Carbamazepine 2. Ethosuximide 3. Phenytoin 4. Lamotrigine

What is the mu opioid receptor responsible for?

physical dependence - euphoria - Resp and CV depression - Constipation - Sedation

What is the kappa opioid receptor responsible for?

- miosis - dysphoria - sedation

What is the delta opioid receptor responsible for?

antidepressant effects

Dextromethorphan

opioid

Which opioids are used for pain control?

1. Morphine 2. Fentanyl 3. Codeine

Which opioids are used as cough suppression?

1. Codeine 2. Dextromethorphan (suppress cough reflex in the brainstem)

Which opioids are used for diarrhea?

Diphenoxylate (analog of meperidine, decreases smooth muscle motility in the gut)

Which opioids are used for acute pulmonary edema?

Morphine- acts to reduce anxiety and cardiac preload

What are the side effects of oioids?

- Cardiac and resp depression - constipation - miosis

Enzyme that converts levodopa to dopamine?

DOPA decarboxylase

Bromocriptine

- partial DA receptor agonist, used in adjunct tx of parkinsonism and hyperprolactinemia

What are the anti-parkinsonism agents?

1. Levodopa/carbidopa 2. Dopamine agonists: amantadine 3. MAO type B inhibitors: selegiline

Sumatriptan and other triptans: MOA

stimulate the presynaptic 5-HT1d receptors, inhibtion of vasodilation and inflammation fo the dura

Sumatriptan: uses

acute treatment of migraines and cluster headaches

Sumatriptan: side effects

coronary vasospasm with resulting chest apin

Buspirone

- acts as a 5-HT1A presynaptic receptor aprtial agonist | - generalized anxiety disorder

Gabapentin

- GABA analogue | - postherpetic neuralgia, partial seizures

Tx of postherpetic neuralgia?

Gabapentin

Pregabalin

- binds to Ca ion channels in the CNS decreasing glutamate and NE release - used for neuropathic pain and fibromyalgia

Tx of choice for Wolf Parkinson white?

Class IA antiarrythmics

What arrythmias do the Class IA tx?

A fibb and V tach

What arrythmias do the IB tx?

Ventricular arrythmias: ventricular fibrillation and v tach

What two antibiotics can cause pseudomembranous colitis?

1. Ampicillin/amoxicillin | 2. Clindamycin

What organisms are not covered by cephalosporins?

LAME: listeria, atypicals, MRSA, and Enterococci

Anastrazole

aromatase inhibitor, suppressing estrogen to postmenopausal levels- use in breast cancer

Edemestane

aromatase inhibitor, suppressing estrogen to postmenopausal levels- use in breast cancer

Letrozole

aromatase inhibitor, suppressing estrogen to postmenopausal levels- use in breast cancer

Danazol

synthetic androgen that acts as partial agonist at androgen receptors used for endometriosis and hereditary angioedema - weight gain, edema, acne, hirsutism, masculinization, decreased HDL levels

Bevacizumab

human mab | interferes with VEGF receptor activation, thereby inhibiting angiogenesis, used in vascular tumors

Alemtuzumab

- antiCD52 - used for CLL - it initiates direct cytotoxic effect through complement fixation and ADCC

Cyproheptadine

first generation histamine antagonist with nonspecific 5-HT1 and 5-HT2 receptor antaonistic properties - use in SSRI overdose

Cimetidine

H2 blocker

Ranitidine

H2 blocker

Famotidine

H2 blocker

Nizatidine

H2 blocker

H2 blockers: MOA, use, tox

MOAL reversible block of histamine H2 receptors use: PUD, gastritis tox: cimetidine = p450 inhibitor, gynecomastia, impotence, can cross BBB and placenta

Which H2 blockers decrease the renal excretion of creatinine?

Cimetidine and Ranitidine

What are side effects of PPIs?

- C diff infection | - hip fractures due to decreased serum Mg with long term use

Bismuth

- binds t ulcer base, providing physical protection to gastric ulcers and allowing HCO3 secretion - requires an acidic envirnoment

Sucralfate

- binds t ulcer base, providing physical protection to gastric ulcers and allowing HCO3 secretion - requires an acidic envirnoment

Misoprotol: MOA and uses

- PGE1 analog, increases production of gastric mucosal barrier and decreased acid production - prevention of NSAID induced ulcer - maintenance of PDA - induces labor

Octreotide: uses

somatostatin analog | use: acute variceal bleeds, acromegaly, VIPoma, carcinoid tumor

What side effect can all antacids cause?

hypokalemia

Infliximab: MOA, use and side effect

monoclonal antibody to TNFalpha use: crohns disease, UC, RA tox: reactivation of latent TB

Sulfasalazine: MOA use and tox

MOA: antibacterial and anti-inflammatory use: UC and crohns Tox: reversible oligospermia, sulfonamide tox

Ondansetron: MOA, use

MOA: 5-HT3 antagonist, central acting anti-emetic Use: vomiting

Metoclopramide: MOA, use, tox

MOA: D2 receptor antagonist, increases tone, contractility and motility of bowel Use: diabetic and post surgery gastroparesis, antiemetic tox: increased parkinsonian effects - interaction with digoxin and diabetic agents

What pt population is contraindicated w Metoclopramide?

1. Small bowel obstruction | 2. Parkinsons disease

Ursodiol

treatment for Primary biliary cirrhosis | - decreases liver synthesis of cholesterol and intestinal absorption of cholesterol

What are the short acting insulins?

1. Lispro 2. Aspart 3. Glulisine

What are the long acting insulins?

1. Glargine | 2. Determir

What are the first generation sulfonylureas?

1. Tolbutamide | 2. Chlorpropamide

What are the second generation Sulfonylurease?

1. Glyburide 2. Glimepriride 3. Glipizide

Tolbutamide

First generation sulfonylurea | - can cause a disulfuram like reaction

Chlorpropamide

First generation sulfonylurea | - can cause a disulfuram like reaction

Glyburide

Second generation sulfonylurea | - can cause hypoglycemia

Glimepiride

Second generation sulfonylurea | - can cause hypoglycemia

Glipizide

Second generation sulfonylurea | - can cause hypoglycemia

MOA of the sulfonylureas

- close K channel in B cell membrane, cell depolarizes causes insulin release via Ca2+ influx

Glitazones: MOA, toxicity

MOA> increases insulin sensitivity by binding to PPAR-y, increasing GLUT4 transporters tox: weight gain, edema, hepatotoxicity and heart failure

What levels increase with Glitazones?

adiponectin!!

Acarbose

- inhibits intestinal brush border alpha glucosidases - delayed sugar hydrolysis and glucose absorption - decreases postprandial hyperglycemia

Miglitol

- inhibits intestinal brush border alpha glucosidases - delayed sugar hydrolysis and glucose absorption - decreases postprandial hyperglycemia

Exenatide

GLP-1 analog, increases insulin and decreases glucagon release

Liraglutide

GLP-1 analog, increases insulin and decreases glucagon release

Propylthiouracil: MOA, use and tox

MOA: blocks peroxidase, inhibitiong the organification of iodide - bocks 5'deiodinase which decreases peripheral conversion of T4 to T3 Use: hyperthyroidism Tox: skin rash, agranulocytosis, aplastic anemia, hepatotoxicity

Methimazole: MOA, use and tox

MOA: blocks peroxidase, inhibitiong the organification of iodide Use: hyperthyroidism Tox: skin rash, agranulocytosis, aplastic anemia, teratogen

Levothyroxine

MOA: thyroxine replacement - hypothyroidism, myxedema tox: arrhythmias, tremors

Triiodothyronin

MOA: thyroxine replacement - hypothyroidism, myxedema tox: arrhythmias, tremors

Demeclocycline: MOA, use, tox

MOA: ADH antagonist use: SIADH Tox: Nephrogenic DI, photosensitivity, abnormal teeth and bone (member of tetracycline family)

What are the two long acting glucocorticoids?

Dexamethasone and Beclomethasone

Dexamethasone

glucocorticoid: decreases the production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2

Beclomethasone

glucocorticoid: decreases the production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2

Traimcinolone

glucocorticoid: decreases the production of leukotrienes and prostaglandins by inhibiting phospholipase A2 and expression of COX-2

Cyclosporine: MOA, use, tox

MOA: binds to cyclophilins blocking the activation fo T cells by inhibiting calcineurin, thus prevents the production of IL-2 Use: suppresses organ rejection after transplantation tox: nephrotoxicity, htn, hyperlipidemia, tremor, gingival hyperplasia, hirsutism

Tacrolimus: MOA, use, tox

MOA: binds to FK binding protein inhibiting calcineurin and secretion of IL-2 use: post immunosupp in organ transplant tox: same as cyclosporine but no gingival hyperplasia

Sirolimus: MOA, use tox

MOA: inhibits mTOR which inhibits T cell proliferation in response to IL-2 Use: used in kidney transplantation Tox: hyperlipidemia, thrombocytopenia, leukopenia

Azathioprine: MOA, use and tox

MOA: antimetbolite precusor of 6-MP that interfferes with metabolism and synthesis of nucleic acids, thus toxic to proliferating lymphocytes Use: kidney transplant and autoimmune disorders Tox: bone marrow suppression, metablized by xanthine oxidase so toxic if given with allopurinol

Muromonab: MOA, use and tox

MOA: mab that binds CD3 on the surface of T cells, blocks cellular interation responsible for signal tranduction for T cells use: kidney transplant Tox: cytokine release syndrome

Thalidomide

anti-angiogenic, decreases TNF-alpha | causes absent limbs

Use of alpha interferon?

Hepatitis B and C, kaposis sacoma, malignant melanoma

Use of Beta interferon?

multiple sclerosis

Use of gamma interferon?

Chronic granulomatous disease and IL-12 receptor deficiecny

Use of Aldesleukin?

recombinant IL-2 | Use: renal cell carcinoma, metastatic melanoma

Filgrastim

Granulocyte colony stimulating factor: used to recover bone marrow after chemo

Sargramostim

Granulocyte macrophage colony stimulating factor | used to recover bone marrow after chemo

Omalizumab

Antibody to IgE | - used to treat severe asthma

Enoxaparin

LMW heparin, acts more on factor Xa

Dalteparin

LMW heparin, acts more on factor Xa

how does heparin lead to increased clearance of TGs?

it releases endothelium bound lipases which encourages the clearance of TGs

HIT?

IgG antibodies against heparin bound to platelet factor 4, this complex activates platelets > thrombosis and thrombocytopenia

Lepirudin

inhibits thrombin, used as an alternative to heparin for anticoagulating patients with HIT

Agatroban

inhibits thrombin, used as an alternative to heparin for anticoagulating patients with HIT

Bivalirudin

inhibits thrombin, used as an alternative to heparin for anticoagulating patients with HIT

tx of heparin overdose?

protamine sulfate

tx of choice for severe pulmonary embolism?

thrombolytics: alteplase, reteplase, tenecteplase

Tx of thrombolytic overdose?

Aminocaproic acid

how does aspirin inhibit cox?

irreversibly by covalent acetylation

MOA of thrombolytics

Alteplase, reteplase, tenecteplase | - directly aid conversion of plasminogen to plasmin which cleaves thrombin and fibrin clots

first sign of ASA overdose?

tinnitus

pH changes in ASA overdose?

resp alkalosis and metabolic acidosis

Clopidogrel

inhibits platelet aggregation by irreversible blocking ADP receptors - prevents glycoprotein IIb/IIIa from binding to fibrinogen

Ticlopidine

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Prasugrel

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Ticagrelor

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Cilostazol

phosphodiesterase III inhibitor, increasing cAMP in platelets, thus inhibiting platelet aggregation and causing vasodilation

Dipyidamole

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Use of Cilostazol and dipyridamole

Intermittent claudication/PAD coronary vasodilation - prevention of stroke or TIA - angina prophylaxis

What are the GpIIb/IIIa inhibitors?

Abciximab Eptifibatide Tirofiban

What drugs cause torsades?

``` Prolong the QT interval: Class IA antiarrhyth Class III antiarrhyth Macrolides Haloperidol Chloroquine Protease inhibitors ```

Tx of choice for torsades?

push IV magnesium

What drug classes have high efficacy?

1. Analgesics 2. Antibiotics 3. Antihistamines 4. Decongestants

What drug classes have a high potency?

1. Chemotherapeutic 2. Antihypertensive 3. Antilipid

nicotinic receptors are ___ channels, muscarinic are what?

``` Nicotinic = ligand gated Na/K channels Muscarinic = G protein coupled receptors ```

Donepezil

anticholinesterase- increases ACh | used in Alzheimers disease

Galantamine

anticholinesterase- increases ACh | used in Alzheimers disease

Rivastigmine

anticholinesterase- increases ACh | used in Alzheimers disease

tropicamide

antimuscarinic used to produce mydriasis

benztropine

antimuscarinic used in parkinsons disease

ipratropium

antimuscarinic used in COPD and asthma

tioptropium

antimuscarinic used in COPD and asthma

oxybutynin

antimuscarinic used to reduce urgency in mild cystitis and reduce bladder spasms

Glycopyrrolate

antimuscarinic used preoperatively to reduce airway secretions

what do you use to tx torsages?

isoproterenol, because it decreases the QT interval via stimulating both B1 and B2 receptors

Phenylephrine

alpha1 and alph2 agonist, used for hypotension, ocular procedures and as a decongestant

Ritodrine

Beta 2 agonist | used to reduce premature uterine contractions, delays labor

why should you never give someone OD on cocaine a beta blocker?

leaves alpha unopposed- leading to generalized vasoconstriction

what are the two alpha 2 agonists?

Clonidine Alpha-methyldopa - use in htn esp with renal disease (doesnt decrease blood flow to the kidney)

which drugs cause a first dose orthostatic hypotension?

alpha 1 antagonists: tamsulosin, prazosin, doxazosin

When do you use phentolamine?

give to patients on MAO inhibitors who eat tyramine containing foods

Mirtazapine

alpha 2 selective blocker | used for depression

what are the partial beta agonists?

pindolol and acebutolol | PAPA

what beta blocker do you use in esophageal varices?

Nadolol