GABA-A NAM
GABA-A receptor negative allosteric modulator
- ↓ inhibitory chloride current
- Lowers the seizure threshold — an adverse effect, not a therapeutic goal
GABA-A NAM (1/2)
- Lowers seizure threshold
- Named sites not shown
- Zinc – physiologic NAM
- Clozapine → seizures (nonsteroidal antiandrogens) → seizures
- ➔ suggested for treatment of idiopathic hypersomnia by American Academy of Sleep Medicine Guidelines (2021)
GABA-A NAM (2/2)
- Bilobalide in ginkgo biloba
Drugs with this mechanism (19)
- Apalutamide — Androgen-receptor antagonist for prostate cancer; GABA-A effects give seizure risk.
- Bilobalide — Ginkgo terpene lactone and a negative modulator at GABA-A.
- Cefepime — Fourth-generation cephalosporin for febrile neutropenia and Pseudomonas.
- Ceftriaxone — Long-acting third-generation cephalosporin; go-to for meningitis, gonorrhea, and pneumonia.
- Ciprofloxacin — Fluoroquinolone with strong Gram-negative and anti-pseudomonal activity; tendon warnings.
- Clarithromycin — Macrolide used in H. pylori and atypical infections; a strong CYP3A4 inhibitor.
- Clozapine — Most effective antipsychotic; used in treatment-resistant cases despite agranulocytosis risk.
- DHEAS — The sulfated, circulating reservoir form of DHEA; a negative modulator at GABA-A.
- Enoxacin — Fluoroquinolone antibiotic; a potent CYP1A2 inhibitor with seizure risk.
- Enzalutamide — Androgen-receptor antagonist for prostate cancer; GABA-A effects give seizure risk.
- Ertapenem — Once-daily carbapenem lacking Pseudomonas coverage; convenient for outpatient IV.
- Clozapine ODT — Orally disintegrating clozapine for patients who cheek or cannot swallow tablets.
- Imipenem — Broad-spectrum carbapenem (with cilastatin); reserved for resistant infections.
- Levofloxacin — Respiratory fluoroquinolone; once-daily coverage including atypical pneumonia.
- Meropenem — Broad-spectrum carbapenem with good CNS penetration; less seizure-prone than imipenem.
- Penicillin V — Oral penicillin, still first-line for strep throat; seizures at high dose or in renal failure.
- Penicillin G — Parenteral natural penicillin for syphilis and susceptible streptococcal infection.
- Clozapine oral suspension — Clozapine oral suspension; same ANC monitoring as the tablets.
- Zinc — Essential trace mineral and NMDA modulator; OTC, used for colds and Wilson disease.
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