Kaplan Review Pharm

ACE Inhibitors

• ACE inhibitors, or Angiotensin-Converting Enzyme inhibitors, are medications for high blood pressure (hypertension) and heart failure
• They help prevent kidney damage in people with diabetes

How ACE Inhibitors Function

• Relax blood vessels, easing the heart's pumping
• Lower blood pressure

Mechanism

• ACE inhibitors block angiotensin-converting enzyme; part of the renin-angiotensin-aldosterone system (RAAS)

Normal RAAS Function

• The kidneys release renin when blood pressure is low
• Renin then triggers angiotensin I production
• ACE converts angiotensin I to angiotensin II
• Angiotensin II then narrows blood vessels and signals the body to retain sodium and water, increasing blood pressure

Function with ACE Inhibitors

• ACE is blocked, therefore less angiotensin II is produced
• Blood vessels stay relaxed and open
• This lowers blood pressure and reduces the heart's workload

Common ACE Inhibitors

• Lisinopril
• Enalapril
• Ramipril
• Captopril
• Benazepril

Side Effects

• Dry cough is a very common side effect
• Other common side effects are high potassium levels, low blood pressure, and dizziness
• Angioedema (swelling of face/lips) is a rare but serious side effect

Psychotherapeutic Drugs: Antidepressants - SSRIs

• Selective Serotonin Reuptake Inhibitors (SSRIs) include Fluoxetine, Sertraline, Citalopram, Paroxetine, Escitalopram
• SSRIs inhibit serotonin reuptake in the synaptic cleft, increasing serotonin availability
• SSRIs treat depression, anxiety disorders, PTSD, and OCD
• Contraindications include MAOI use within 14 days and severe liver dysfunction
• Adverse effects include sexual dysfunction, insomnia, GI upset, and serotonin syndrome

Psychotherapeutic Drugs: Antidepressants - TCAs

• Tricyclic Antidepressants (TCAs) include Amitriptyline, Nortriptyline, and Imipramine
• TCAs inhibit reuptake of norepinephrine and serotonin
• TCAs treat depression, neuropathic pain, and migraine prophylaxis
• Contraindications include cardiac arrhythmias and MAOIs
• Adverse effects include anticholinergic effects, cardiac toxicity, and orthostatic hypotension

Antipsychotics: Typical (1st Gen)

• Typical antipsychotics include Haloperidol and Chlorpromazine
• They function as Dopamine D2 receptor antagonists
• Typical antipsychotics treat schizophrenia and acute psychosis
• Contraindications: Parkinson’s disease, severe CNS depression
• Adverse Effects: Extrapyramidal symptoms (EPS), tardive dyskinesia, and sedation

Antipsychotics: Atypical (2nd Gen)

• Atypical antipsychotics include Risperidone, Olanzapine, Quetiapine, and Clozapine
• They function as Dopamine and serotonin (5-HT2A) receptor antagonists
• They treat schizophrenia and bipolar disorder
• Contraindications include seizure disorders (especially Clozapine) and agranulocytosis
• Adverse effects include weight gain, diabetes risk, and agranulocytosis (Clozapine)

Antibiotics: Penicillins

• Penicillins include Amoxicillin, Penicillin G, and Ampicillin
• They inhibit bacterial cell wall synthesis
• They treat strep throat, syphilis, and respiratory infections
• Penicillin allergy is a contraindication
• Adverse effects include allergic reactions, GI upset, and rash

Antibiotics: Cephalosporins

• Cephalosporins include Cefazolin, Ceftriaxone, and Cephalexin
• They function similar to penicillins by inhibiting cell wall synthesis
• Cephalosporins treat pneumonia, UTIs, and are used for surgical prophylaxis
• Severe penicillin allergy is a contraindication
• Adverse effects include GI upset, hypersensitivity, and superinfection

Antibiotics: Macrolides

• Macrolides include Azithromycin and Erythromycin
• They inhibit bacterial protein synthesis (50S ribosome)
• They treat atypical pneumonia, chlamydia, and strep infections
• Liver disease is a contraindication
• Adverse effects include QT prolongation and GI upset

Antibiotics: Aminoglycosides

• Aminoglycosides include Gentamicin and Tobramycin
• They inhibit bacterial protein synthesis (30S ribosome)
• They treat serious Gram-negative infections
• Myasthenia gravis is a contraindication
• Adverse effects include nephrotoxicity and ototoxicity

Chemotherapy Drugs: Alkylating Agents

• Alkylating agents include Cyclophosphamide and Ifosfamide
• They cross-link DNA, preventing replication
• They treat breast cancer, lymphomas, and leukemia
• Severe bone marrow suppression is a contraindication
• Adverse effects include myelosuppression and hemorrhagic cystitis

Chemotherapy Drugs: Antimetabolites

• Antimetabolites include Methotrexate and 5-Fluorouracil (5-FU)
• They interfere with DNA/RNA synthesis
• They treat leukemia, breast cancer, and colon cancer
• Liver dysfunction and pregnancy are contraindications
• Adverse effects include mucositis, bone marrow suppression, and hepatotoxicity

Chemotherapy Drugs: Plant Alkaloids

• Plant alkaloids include Vincristine and Paclitaxel
• They inhibit mitosis by interfering with microtubules
• They treat leukemia, lymphoma, and breast cancer
• Neuropathy is a contraindication
• Adverse effects include neurotoxicity and constipation

Anticonvulsants: Sodium Channel Blockers

• Sodium channel blockers include Phenytoin, Carbamazepine, and Lamotrigine
• They stabilize neuronal membranes by blocking voltage-gated sodium channels
• They treat focal and generalized seizures
• Heart block and liver disease are contraindications
• Adverse effects include rash (SJS with Lamotrigine), gingival hyperplasia (Phenytoin), and ataxia

Anticonvulsants: GABA Enhancers

• GABA enhancers include Valproic acid, Phenobarbital, and Clonazepam
• They enhance GABA (inhibitory neurotransmitter)
• They treat generalized seizures, anxiety, and mood stabilization
• Liver disease and pregnancy (Valproate—teratogenic) are contraindications
• Adverse effects include hepatotoxicity, sedation, and weight gain

Anticonvulsants: Calcium Channel Modulators

• Calcium channel modulators include Ethosuximide (T-type) and Gabapentin (high-voltage calcium channels)
• They reduce neuronal excitability via calcium channel modulation
• They treat absence seizures (Ethosuximide) and neuropathic pain (Gabapentin)
• Renal impairment (Gabapentin) is a contraindication
• Adverse effects include sedation, dizziness, and GI upset