Pharmacology8-2 Flashcards
What is the mechanism of action for a benzodiazepine?
Benzo’s bind to the GABA-A receptor-chloride channels in the CNS and increase the frequency at which they open.
This results in: (1) anxiolytic (2) anticonvulsant (3) muscle relaxant & (4) sedative-hypnotic effects
Glanzmann thrombasthenia is a rare bleeding disorder that typically presents in childhood with mucocutaneous bleeding. Peripheral blood smear would show no platelet clumping. What type of anti-coagulation drugs most closely mimic Glanzmann thrombasthenia?
Individuals with GT lack a functional glycoprotein IIb/IIIa platelet surface receptors. Anti-coagulant drugs that block the GPIIb/IIIa receptor (i.e Abciximab) would most closely resemble this illness.
Treatment:
Mycobacterial infection in a patient on HAART
Rifabutin
Typically, rifampin is used for mycobacterial infections; however, in patients concurrently taking a protease inhibitor, rifampin is contraindicated due to it’s ability to induce the activity of P-450. Rifampin would result in decreased serum levels of protease inhibitor.
What are the shared side effects of protease inhibitors?
(-avir)
- Lipodystrophy
- Hyperglycemia
- Inhibition of P-450
Each protease inhibitor has additional side effects. For example, idinavir also causes nephrotoxicity and nephrolithiasis.
Which organisms are not covered by cephalosporins?
The LAME ones. (1) Listeria (2) Atypicals (chlamydia & Mycoplasma) & (3) Enterococci
Mechanism of Action:
Penicillins
- covalently bind the active site of transpeptidase
- prevent crosslinking of peptidoglycan cell wall
- weak cell wall integrity causes osmotic lysis of the bacterium
Penicillins are structural analogs of D-Ala-D-Ala.
Diagnosis:
Your patient has a history of schizophrenia, treated with risperidone, and presents with (1) breast tenderness & (2) no menstrual periods for 3 months
Drug induced amenorrhea
Risperidone is an atypical antipsychotic. Many antipsychotics cause hyperprolactinemia due to their anti-dopaminergic actions
Pathogenesis:
Risperidone induced amenorrhea
- Risperidone is an antipsychotic with anti-dopaminergic actions.
- Decreased dopamine releases the inhibitory break on prolactin production.
- Excess prolactin will shut down the HPA axis, preventing the production of GnRH, LH & FSH.
Why might you consider prescribing a beta blocker to a patient on a anti-psychotic?
Anti-psychotic medications have some side effects: (1) Extrapyramidal side effects (2) Tardive dyskinesia & (2) Neuroleptic malignant syndrome. The beta-blocker would be helpful for a patient experiencing akathisia, a extrapyramidal side effect.
What the extrapyramidal side effects associated with anti-psychotic usage?
(1) Extrapyramidal side effects: acute dystonic reaction, akathisia & drug-induced parkinsonism
(2) Tardive dyskinesia
(3) Neuroleptic malignant syndrome
Mechanism of Action:
Carbamazepine
blocks voltage gated Na channels in cortical neurons
Side effects: (1) Bone marrow suppression (2) hepatoxicity & (3) SIADH
Carbamazepine may be used to treat: (1) simple partial (2) complex partial & (3) tonic-clonic seizures
Treatment:
Status epilepticus
- IV lorazepam (simultaneously load phenytoin)
- Phenobarbital if refractory
- Intubation and general anesthesia if still refractory
Function:
Phenytoin
Phenytoin inhibits neuronal firing by reducing the ability of the sodium channels to recover from inactivation. Thus, at high frequency firing rates, the neuron is refractory to reactivation an seizure activity is reduced.
Why are benzodiazepines first line therapy for status epilepticus over phenytoin?
Benzodiazepines have a rapid onset of action. Phenytoin takes approximately 15 minutes.
Name that antifungal!
Alters the fungal cell membrane composition by inhibiting the demethylation of lanosterol into ergosterol
(-azoles) Ketoconazole, fluconazole, itraconazole, voriconazole
This drugs also increase the serum concentration of drugs metabolized by liver P-450 enzymes like: warfarin, cyclosporine, tacrolimus, phenytoi, isoniazid, rifampin, oral hypoglycemics and others.
Name that antifungal!
Causes pore formation and ultimately lysis by binding ergosterol in the fungal cell membrane
Polyene antifungals (i.e. Amphotericin B & nystatin)
Name that antifungal!
Decreases the synthesis of ergosterol by inhibiting the fungal enzyme squalene-2, 3, epoxidase
Terbinafine
Terbinafine is used to treat dermatophytoses as it accumulates in the skin and nails.
Name that antifungal!
Inhibits fungal mitosis by binding polymerized microtubules and disrupting the fungal mitotic spindle
Griseofulvin
Griseofulvin is only effective for dermatophytosis because it accumulates in the skin and appendages.
How do cholinomimetics affect the smooth muscle tone of the detrusor muscle in the bladder?
Cholinomimetics would cause contraction of the detrusor muscle and promote urination.
Which anticonvulsant is most commonly used for seizure prophylaxis?
Valproate (Valproic acid)
What drug is indicated to treat (1) major depression (2) obsessive-compulsive disorder & (3) anxiety disorders?
Sertraline (SSRI)
Do not prescribe sertraline to a bipolar person. It may induce mania.