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Glossary of Kyle's Drugs

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Created by kmcyoder

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Metronidazole

- MOA
- clinical use
- Adverse effects



MOA: forms toxic metabolites in bacterial cell that damage DNA

Clinical use: GET GAP at the Metro!

Giardia
Entamoeba
Trichomonas
Gardnerella vaginalis
Anaerobes (bacteroides, Clostridium)
H. Pylori - "triple therapy"

Adverse effects: Disulfiram-like rxn with EtOH, metallic taste










Lorazepam

Class
MOA
Use
Adverse effects




Class: Benzodiazepine

MOA: binds GABA receptors (Cl- channels) on neurons which increase affinity for GABA and causes hyperpolarization of membrane

Use: anxiety, insomnia, sedation, status epilepticus

Adverse effects: drowsiness, DO NOT USE WITH ETOH





Diazepam

Class:
MOA:
Use:
Adverse effects:




Class: Benzodiazepines

MOA: binds to GABA receptors (Cl- channels) on neurons which increases affinity for GABA and hyperpolarization of the membrane

Use: anxiety, status epilepticus, muscle spasm, sedation

Adverse effects: drowsiness, physical and psychological dependence





Carbamazepine

Class:
MOA:
Use:
Adverse effects:




Class: anticonvulsant
MOA: blocks Na+ channels in CNS neurons which decreases firing of ectopic foci
Use: partial seizures and tonic-clonic seizures; bipolar disorder, neuropathic pain
Adverse Effects:Ataxia, drowsiness, blurry vision, Rare blood dyscrasias: agranulocytosis, aplastic anemia, thrombocytopenia




Valproate

Class:
MOA:
Use:
Adverse effects:




Class: anticonvulsant
MOA: Na+ channel blockade, GABA transaminase blockade and action at T-type Ca2+ channels
Use: simple and complex absence seizures, tonic-clonic seizures, migraine prevention, manic phase of bipolar disorder
Adverse effects: N/V, dizziness, sedation


Fluoxetine

Class:
MOA:
Use:
Adverse effects:




Class: SSRI
MOA: inhibits the reuptake of serotonin (DO NOT Block the muscarinic, alpha-receptors, and histaminic H1 receptors like TCAs so there are fewer side effects)
Use: depression, OCD, bulimia, anorexia, fibromyalgia, panic attacks, phobia, PMDD
Adverse Effects: anxiety, drowsiness, insomnia, sexual dysfunction, CYP inhibitor


Lithium

Class:
MOA:
Use:
Adverse effects:




Class: mood stabilizer

MOA: uncertain; possibly decreased noradrenergic neurotransmission by interfering with the PIP2 second messenger system leading to its depletion in neuronal membranes of the CNS

Use: bipolar disorder

Adverse effects: HA, dry mouth, polydipsia, polyuria (essentially diabetes insipidus), polyphagia, GI distress





Ranitidine, cimetidine, famotidine

Class:
MOA:
Use:
Adverse effects:




Class: H2 blocker

MOA: blocks H2 receptors on gastric parietal cells to reduce gastric acid secretion

Use: PUD, GERD, dyspepsia

Adverse effects: few
Cimetidine - potent CYP450 inhibitor, loss of libido, gynecomastia






Omeprazole, esomeprazole, pantoprazole

Class:
MOA:
Use:
Adverse effects:




Class: PPI

MOA: irreversibly inhibits H/K ATPase in gastric parietal cells to prevent gastric acid secretion

Use: PUD, GERD, Zollinger-Ellison, dyspepsia, H. pylori infection

Adverse effects: Abdominal pain, drug interactions





Tamoxifen

Class:
MOA:
Use:
Adverse effects:




Class: antineoplastic drug/SERM

MOA: competes with estrogen for receptors in breast tissue to suppress cancer growth; partial agonist of bone and endometrium

Use: breast cancer treatment and prophylaxis

Adverse effects: nausea, hot flashes, menstrual irregularities





Raloxifene

Class:
MOA:
Use:
Adverse effects:




Class: SERM

MOA: agonist of receptors on bone to reduce bone resorption; antagonist of receptors on breast and endometrium

Use: osteoporosis in postmenopausal women

Adverse effects: hot flashes





Methotrexate

Class:
MOA:
Use:
Adverse effects:




Class: folate reductase inhibitor/antineoplastic agent

MOA: inhibits dihydrofolate reductase which prevents formation of nucleotide bases for DNA synthesis; S-phase specific

Use: all kinds of cancers, RA, ectopic pregnancy

Adverse effects: N/V, mucositis, hepatotoxicity, myelosuppression





5-Fluorouracil

Class:
MOA:
Use:
Adverse effect:




Class: Antineoplastic agent/pyrimidine antimetabolite

MOA: converted to a pyrimidine analog which inhibits thymidylate synthase

Use: many cancers

Adverse effects: D/V, mucositis, myelosuppression, rash





6-mercaptopurine

Class:
MOA:
Use:
Adverse effects:




Class: antineoplastic agent/purine antimetabolite

MOA: converted to nucleotide triphosphate by HGPRTase and inhibits de nove purine synthesis

Use: leukemias

Adverse effects: myelosuppression, hepatotoxicity, hyperuricemia





Cytarabine (ara-C)

Class:
MOA:
Use:
Adverse effects:




Class: antineoplastic agent/antimetabolite

MOA: deoxycytidine analog that is converted eventually to ara-CTP that competitively inhibits DNA polymerase

Use: leukemias

Adverse effects: myelosuppression





Cyclophosphamide

Class:
MOA:
Use:
Adverse effects:




Class: alkylating agent/nitrogen mustard

MOA: cross links DNA at guanine residues (N-7) which prevents DNA replication and transcription; requires CYP enzymes for activation

Use: cancer

Adverse effects: hemorrhagic cystitis, myelosuppression





Carmustine, lomustine, streptozocin

Class:
MOA:
Use:
Adverse effects:




Class: nitrosurea/alkylating agent

MOA: cross links DNA by binding guanine residues and prevents DNA replication/transcription

Use: cancer

Adverse effects: CNS toxicity, pulmonary fibrosis, myelosuppression





Cisplatin

Class:
MOA:
Use:
Adverse effects:




Class: antineoplastic agent

MOA: forms reactive metabolites that bond DNA and cross link strands and break strands

Use: cancer

Adverse effects: nephrotoxicity, acoustic nerve damage





Busulfan

Class:
MOA:
Use:
Adverse effects:




Class: alkylating agent

MOA: cross links DNA at guanine bases and prevents replication/transcription

Use: CML

Adverse effects: pulmonary fibrosis, myelosuppression, GI disturbances





Doxorubicin

Class:
MOA:
Use:
Adverse effects:




Class: antibiotic antineoplastic agent

MOA: generates free radicals using iron that breaks strands

Use: cancers

Adverse effects: colors urine red, cardiotoxicity, myelosuppression, alopecia





Bleomycin

Class:
MOA:
Use:
Adverse effects:




Class: antineoplastic antibiotic/intercalating agent

MOA: complexes iron-forming free radicals that cause DNA strand breaks

Use: cancer

Adverse effects: pulmonary fibrosis, mucositis, myelosuppression





Vincristine

Class:
MOA:
Use:
Adverse effects:




Class: vinca alkaloid/mitotic inhibitor

MOA: binds beta-subunit of tubulin and prevents polymerization of microtubules (mitotic spindles); M-phase specific

Use: cancer

Adverse effects: peripheral neuropathy, alopecia, N/V





Paclitaxel

Class:
MOA:
Use:
Adverse effects:




Class: mitotic inhibitor

MOA: binds tubulin and prevents depolymerization of mitotic spindles; M-phase specific

Use: cancer

Adverse effects: arthralgias, peripheral neuropathy, alopecia, myelosuppression





Trimethoprim-Sulfamethoxazole (BACTRIM)

Class:
MOA:
Use:
Adverse effects:




Class: folate antagonist

MOA: PABA analog that inhibits folate synthesis in bacteria; inhibits dihydrofolate reductase and prevents nucleotide synthesis

Use: Respiratory infection, diarrhea by gram-negatives, UTIs, prophylaxis in AIDS patients

Adverse effects: N/V, myelosuppression in AIDS patients, hypersensitivity





Azithromycin, clarithromycin, erythromycin

Class:
MOA:
Use:
Adverse effects:




Class: Macrolide

MOA: binds 50s ribosomal subunit and prevents protein synthesis

Use: Gram positive respiratory infections, otitis media, second-line for MRSA, atypical bacteria coverage - Legionella, Chlamydia, Mycoplasma

Adverse effects: GI upset, prolonged QT syndrome (erythromycin)





Cephalexin, cephalothin, cephapirin, cephradine (others with ph remember you must get a PhD first - generation), cefazolin (don't let this faz you)

Class:
MOA:
Use:
Adverse effects:




Class: Second-generation cephalosporin; beta-lactam antibiotic

MOA: binds penicillin-binding protein to prevent transpeptidation reaction in bacterial cell wall synthesis

Use: Gram-positive cocci, few gram-negative

Adverse effects: rash, diarrhea, pseudomembranous colitis





Ciprofloxacin

Class:
MOA:
Use:
Adverse effects:




Class: fluoroquinolone

MOA: inhibits bacterial DNA gyrase (topoisomerase II) and topoisomerase IV to prevent DNA replication

Use: UTI, skin infections, gonorrhea, infectious diarrhea

Adverse effects: diarrhea, nausea, insomnia, damage cartilage so use with caution in children





Levofloxacin

Class:
MOA:
Use:
Adverse effects:




Class: fluoroquinolon

MOA: inhibits bacterial DNA gyrase and topoisomerase IV to prevent DNA replication

Use: community-acquired pneumonia, Pseudomonas aeruginosa, Chlamydia, Mycoplasma

Adverse effects: diarrhea, nausea, insomnia, damage to cartilage use with caution in children





Phenelzine, tranylcypromine

Class:
MOA:
Use:
Adverse effects:




Class: MAOI

MOA: inhibits monoamine oxidase which increases CNS levels of norepinephrine and serotonin

Use: atypical depression, anxiety

Adverse effects: dizziness, insomnia, orthostatic hypotension, very dangerous when taken with other antidepressants





Amitriptyline, nortriptyline, clomipramine (OCD), desipramine, imipramine (bed-wetting)

Class:
MOA:
Use:
Adverse effects:




Class: Tricyclic antidepressant agent

MOA: blocks the reuptake of serotonin and norepinephrine; also blocks muscarinic and alpha-receptors

Use: depression, chronic pain

Adverse effects: sedation, tachycardia, urinary retention, constipation, overdose causes Convulsions, Coma and Cardiotoxicity





Thioridazine, chlorpromazine

Class:
MOA:
Use:
Adverse effects:




Class: Typical antipsychotic - low potency

MOA: blocks D2 receptors in limbic region, basal ganglia; blocks muscarinic receptors

Use: psychotic disorders - schizophrenia (only positive symptoms)

Adverse effects: extrapyramidal signs (acute dystonia, parkinsonian symptoms, restlessness, tardive dyskinesia), neuroleptic malignant syndromes





Haloperidol, trifluoperazine, fluphenazine, droperidol

Class:
MOA:
Use:
Adverse effects:




Class: Typical antipsychotic - high potency

MOA: blocks D2 receptors in limbic area, basal ganglia; blocks muscarinic and alpha-receptors

Use: schizophrenia, Tourette's syndrome, psychosis

Adverse effects: extrapyramidal signs (acute dystonia, parkinsonian symptoms, restlessness, tardive dyskinesia), constipation, dry mouth





Olanzapine, clozapine, aripiprazole, ziprasidone, quetiapine

Class:
MOA:
Use:
Adverse effects:




Class: atypical antipsychotics

MOA: blocks serotonin receptors > D2 receptors in CNS, also block histamine, muscarinic and alpha-receptors

Use: schizophrenia (Positive and negative symptoms), manic phases of bipolar disorder

Adverse effects: fewer extrapyramidal signs compared to typical antipsychotics, Clozapine-agranulocytosis, sedation, dry mouth





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