Term
| antibiotics that inhibit cell wall synthesis |
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Definition
beta lactams: penicillin, cephalosporins
gram (+) bacteria |
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Term
| Penicilin is bacteriostatic or bactericidal? |
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Definition
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Term
| Inhibitors of DNA synthesis and Integrity |
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Definition
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Term
| Inhibitors of Transcription and Translation |
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Definition
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Term
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Definition
Competitive inhibitors of D-alanine in rxn with transpeptidases in the final step of bacterial cell wall synthesis.
Nucleophilic attack on carboxyl in penicillin by hydroxyl in PBP
The bond between nitrogen and carboxyl is broken
Penicillin is covalently bound to the enzyme blocking its action, cell wall synthesis
Specific for gram (+). Gram (+) have larger cell wall. |
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Term
| 2nd mechanism of penicillins |
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Definition
Activation of the enzyme muramyl synthase
Muramyl synthase separates daughter cells after cell division
Activation in the absence of cell division causes lysis of cell wall: a suicide mechanism |
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Term
| Pen V spectrum and indications |
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Definition
Spectrum: Gram+ Cocci, Gram+ Rods, Most oral anaerobes
Indications- soft tissue infections, cellulitis, pulpal origin infections |
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Term
| Augmentin (Amoxicillin and Clavulanic Acid) |
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Definition
Forms covalent bond to b-lactamase active site (suicide inhibitor)
Not recommended for the treatment of routine oral infections
Prescribed for bacterial infections expressing b-lactamase
Zosyn (piperacillin/tazobactam) used for Pseudomonas aeruginosa |
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Term
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Definition
Semi synthetic penicillins that are resistant to beta lactamase
Culture and sensitivity tests should be performed before prescribing these medications
There are species of staphylococci that are resistant to these drugs
Ineffective against chromosomally mediated beta lactamases found in Enterobacter, Pseudomonas aeruginosa
And organisms producing inducible extended spectrum beta lactamases |
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Term
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Definition
Most common symptom is maculopapular or urticarial skin reactions
Most common cause of death by anaphylaxis (75 %) in US 400-800 deaths/year
1-10 % of population is allergic to penicillin increases with age
Risk Factors: multiple allergies, asthma, allergic rhinitis, elderly |
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Term
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Definition
Modified beta lactam antibiotics
Comparable to PCN, but with an extended range
4 generations: Each generation increases spectrum against gram negative bacilli while becoming less effective against gram positive rods |
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Term
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Definition
2nd generation: anti-staphylococcal activity, gram negative, anaerobes
Antacids decrease absorption |
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Term
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Definition
| 1st generation: gram positive aerobes, facultative cocci, methicillin-sensitive Staph. aureus (MSSA) |
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Term
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Definition
| 3rd generation: gram negative, PCN resistant Strep. pneumoniae, Pseudomonas |
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Term
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Definition
| 4th generation: Pseudomonas, methicillin-resistent Staph. aureus (MRSA), hyper b-lactamase organisms |
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Term
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Definition
About 1 % of population is allergic to cephalosporins
The issue of cross sensitivity to cephalosporin and PCNs is unresolved.
PCN allergic individuals have a 4-fold greater risk of allergy to cephalosporin
But they have a 3-4 times risk of being allergic to any drug |
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Term
| Cephalosporin: Drug Interactions |
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Definition
Antacids decrease absorption of cefaclor
Nephrotoxic
Bacteriostatic antibiotics interfere with the bactericidal effects of cephalosporins
tetracycline, erythromycin, clindamycin |
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Term
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Definition
Mechanism: Prevent DNA supercoiling
Topoisomerase nicks double stranded DNA and seals the nicked DNA
DNA gyrase guides the passage of DNA through the enzyme complex
Stabilization of DNA enzyme complex after nicking and before resealing
Use in dentistry: culture and sensitivity test
Management of refractory or rapidly progressive periodontitis |
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Term
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Definition
2nd generation Fluoroquinolone
Increase CNS toxicity with NSAIDS
Reduces the hepatic clearance of warfarin
Cimetidine (Tagamet) increases blood levels of Cipro
Antacids and sucralfate decreases absorption
Adverse effects: N+V, Heartburn, Headache, dizziness, Rash, sunburn, Arthralgia, joint swelling |
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Term
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Definition
Often prescribed to patients with known penicillin allergies
Erythromycin: base, stearate, ethylsuccinate
Clarithromycin
Azithromycin (Zithromax)
Lincosamides: Clindamycin |
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Term
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Definition
Reversibly bind to the P site of the 50S ribosomal subunit and inhibits translocation of ribosome along mRNA
Inhibit RNA-dependent protein synthesis
Stimulate the dissociation of peptidyl t-RNA from the ribosome
Fat soluble
Bacteriostatic |
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Term
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Definition
Macrolides: tetracycline, clindamycin
Selective uptake by phagocytic cells
These cells are drug delivery vehicles of the drug to sites of inflammation and infection
Tissue concentrations of Azithromycin may reach 100 times that of serum.
Post-antibiotic effects: Tissue concentration exceeds MIC for days after plasma levels have dropped. |
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Term
| Macrolides and Clindamycin |
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Definition
Spectrum: aerobic and anaerobic gram+ cocci, pneumococci, staphylococci
Also active against: Mycoplasma, Legionella, Chlamydia, Helicobacter, and some mycobacteria |
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Term
| Clarithromycin and Azithromycin dosage |
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Definition
Clarithromycin dose: 250-500 mg q12h for 7-10 days
Azithromycin dose: 500 mg on day 1, 250 mg qd days 2-5
Clarithromycin and Azithromycin cause less GI upset than erythromycin |
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Term
| Erythromycin and Clarithromycin drug interactions |
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Definition
Inhibit p450 enzymes, many drug interactions
Carbamazepine
Theophylline
Benzodiazepines
Cyclosporin and tacrolimus
HMG-CoA Inhibitors
Methylprednisolone
Statins
Clarithromycin and Azithromycin cause less GI upset than erythromycin
Azithromycin: No effect on the p450 enzymes |
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Term
| Macrolide Antibiotic Resistance |
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Definition
Transport from the cell
Phosphorylation and glycosylation of the drugs
Reduced macrolide binding by demethylation of a residue on the 23S ribosomal RNA transferase region |
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Term
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Definition
Mechanism: Similar to macrolides, binds to the 50 S subunit of the ribosome
Spectrum: aerobic gram + cocci, some anaerobic gram -/+ organisms
Good penetration into bone and soft tissue
Indications: Prevention of bacterial endocarditis in patients allergic to PCN and orofacial infections that can’t be eradicated by PCN |
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Term
| Clindamycin: Adverse Effects and Drug Interactions |
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Definition
GI upset and diarrhea
Most serious: Pseudomembranous Colitis
Drug Interaction: Absorption inhibited by kaolin-pectin (Kaopectate) antidiarrheal drugs |
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Term
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Definition
Bacteriostatic
Erythromycin and Clarithromycin : Many drug interactions
Resistance is associated with tetracycline resistance also
Clindamycin is the alternate for prophylaxis when pt is allergic to PCN |
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Term
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Definition
Mechanism: In sensitive anaerobes, the nitro group is reduced to metabolites that inhibit DNA polymerase
Bactericidal
Highly effective against gram– anaerobes
and protozoan parasites (giardiasis, amoebiasis, tricomoniasis,
Serious acute orofacial infections
Management of refractory/rapidly progressive periodontitis |
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Term
| Metronidazole (Flagyl) resistance |
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Definition
Reduction in activity or expression of genes that control nitroreductase activity
Reduces concentration of active metabolites of metronidazole
Most commonly seen in H. pylori |
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Term
| Metronidazole (Flagyl) drug interactions and adverse effects |
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Definition
Metronidazole increases the levels of:
Lithium
Warfarin
Phenytoin
Cimetidine decreases the liver metabolism of metronidazole
Phenobarbital may reduce its effectiveness
N+V, Disulfiram rxn with EtOH: flushing, tachycardia, N+V, psychosis, Metallic taste, Dark red or brown urine |
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Term
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Definition
Class: Oxazolidinone
Spectrum: Aerobic Gram-positive bacteria, Gram-negative bacteria, anaerobic bacteria
Mechanism: Binds to a site on the bacterial 23S ribosomal RNA of the 50S subunit and prevents the formation of a functional 70S initiation complex
Bacteriostatic against enterococci and staphylococci; bactericidal against streptococci |
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Term
| Linezolid (Zyvox) adverse affects and resistance |
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Definition
Adverse Effects: Oral candidiasis, taste alteration, and tongue discoloration, headache, diarrhea, nausea (short term use). Long term use: bone marrow suppression, thrombocytopenia
Has mild MAO inhibitor properties
Resistance: Point mutation in the 23S rRNA (substitution of thymine for guanine at position 2576) |
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Term
| Linezolid (Zyvox) contraindications |
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Definition
Serotonin reuptake inhibitors, tricyclic antidepressants, serotonin 5-HT1 receptor agonists, meperidine, or buspirone
Serotonin syndrome |
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Term
| Acetaminophen contraindications |
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Definition
liver disease, hepatitis, and alcoholism.
4g/day max
2.6g/day for kids |
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Term
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Definition
impaired pulmonary function, head injuries, endocrine disease, hepatic function impairment, seizure disorders, pregnancy, and a history of drug abuse or alcoholism
any drugs that depress CNS function, such as, antidepressants, antipsychotics, and benzodiazepines, should be used cautiously with opiates to avoid the heightened risk of CNS depression.
Thiazide increase risk of orthostatic hypeotension |
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Term
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Definition
Angiotensin Receptor An"tan"gonist
Pharmacological Effects:
Inhibit vasoconstriction
Inhibit aldosterone secretion
Inhibit sodium retention |
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Term
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Definition
| Angiotensin Converting Enzyme (ACE) Inhibitor |
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Term
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Definition
Indications: Hypertension, Heart failure, MI
Pharmacological Effects:, Decrease concentrations of ATII,
(vasodilation), Increase bradykinin (a vasodilator),
Decrease aldosterone |
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Term
| NSAIDs AND aspirin inhibit anti-HTN effects of |
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Definition
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Term
| ACE inhibitor adverse effects |
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Definition
Adverse Effects:
Altered or reduced taste sensation
Hypotension
Bradykinin by inhibiting its degradation-
(vasodilation and bronchoconstriction)
Cough in 20% of patients
Angioedema of the face and mouth (more common in African American patients) |
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Term
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Definition
Indications: Heart Failure, Hypertension, MI, Prevention of stroke
Comparison to ACE Inhibitors
Less adverse rxns (cough and angioedema)
Less effective vasodilation |
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Term
| Angiotensin receptor an"tan"gonist drug interactions |
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Definition
Increase in anti-HTN effect with fluconazole and ketoconazole
Increase renal toxicity with NSAIDs |
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Term
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Definition
α1 antagonist
α1 receptor blockade
smooth muscle relaxation
decrease in Total Peripheral Resistance |
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Term
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Definition
| inhibit HMG CoA reductase which is in the pathway of the production of cholesterol. This is done in the liver. As the liver starts to reduce the amount of cholesterol that it makes, the body will increase its expression of LDL receptors to help clear the cholesterol from the blood. |
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Term
| HMG CoA adverse effects and interactions |
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Definition
Adverse Effects:
Rhabdomyolysis leading to kidney failure
Constipation, diarrhea, stomach pain, nausea
Drug Interactions:
EtOH increase levels and rhabdomyolysis
Erythromycin, itraconazole, ketoconazole
contraindicated with Mevacor (Lovastatin)
used with caution in others because of increase chance of rhabdomyolysis. |
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Term
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Definition
Cholesterol absorption inhibitor
Mechanism: Selectively inhibits cholesterol uptake through a brush border protein (NPC1L1)
PCOL Effects
↓cholesterol absorption by 50%
↓LDL concentration in the plasma
↓cholesterol content of chylomicrons
Side Effects: Abdominal pain, diarrhea
Contraindicated in hepatic impairment |
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Term
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Definition
MOA: irreversible inhibitor of platelet aggregation (covalent modifier of P2Y12 ADP receptor)
INDICATION: secondary prevention of MI, stroke, peripheral vascular disease; coronary artery stents; coronary artery bypass grafting
PHARM EFFECTS: inhibits sustained platelet aggregation (transient aggregation can still occur)
NOTES: elective procedures should be deferred until pt has completed appropriate course of clopidogrel therapy (12 mo after drug-eluting stent implantation or 1 mo for bare-metal stent) |
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Term
| dipyridamole (Persantine) |
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Definition
MOA: inhibitor of phosphodiesterase (an enzyme which degrades cAMP; high [cAMP] leads to a decrease in platelet aggregation)
INDICATION: ADJUNCT -- used with warfarin in prosthetic heart valve replacement; used with ASA to reduce stroke risk
PHARM EFFECTS: increase in [cAMP] leading to decrease in platelet aggregation
ADVERSE EFECTS: gingival bleeding |
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Term
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Definition
MOA: irreversible nonselective inhibitor of COX, thereby inhibiting thromboxane A2 (TXA2) formation which is a potent inducer of platelet aggregation
INDICATION: prevention of arterial thrombosis (stroke, MI, TIA)
PHARM EFFECTS: reduction in clotting inducer TXA2
ADVERSE EFECTS: gastric ulcer
NOTES: 4-10 days to recover platelet aggregation following ASA discontinuation |
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Term
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Definition
MOA: inhibitor of vit K epoxide reductase (vit K is a cofactor for synthesis of many clotting factors)
ADVERSE EFECTS: too much: bleeding; too little: angina, blood clots
CONTRAINDICATIONS: extensive drug interactions-
NOTES: pt must avoid vit K in diet (primarily leafy greens); INR every 2 weeks
no need to abruptly discontinue warfarin prior to common dental procedures; risk of life-threatening bleeding < risk of thrombembolic event
aim for INR < 3.0
40 h half-life
can be reversed with vit K in case of emergency |
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Term
heparin
enoxaparin (Lovenox) |
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Definition
MOA: binds to and activates antithrombin III which itself covalently binds to serine protease and prevents it from participating in coagulation cascade --> inactivates thrombin, factors IXa, Xa, Xia, XIIa
INDICATION: "used by patients at home as a 'bridge to warfarin'"
PHARM EFFECTS: efficient inactivation of Xa as well as thrombin, Ixa, Xia, & XIIa
NOTES: AT III inhibits clotting; heparin binds ATIII and speeds up the anti-clotting reaction 1000x |
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Term
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Definition
MOA: direct thrombin inhibitor
INDICATION: reduces risk for stroke in pts w/ atrial fibrillation
NOTES: unlike warfarin, there is no reversal agent due to its MOA. 14 h half-life compared to warfarin's 40 h half-life; therefore, a missed dose is more serious |
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Term
atorvastatin (Lipitor)
"statin" |
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Definition
MOA: competitively inhibits HMG-CoA reductase
INDICATION: hyperlipidemia
PHARM EFFECTS: inc in synthesis of hepatic LDL receptors; inc in hepatic uptake of LDL and ID
ADVERSE EFECTS: rhadbomyolysis leading to kidney failure; constipation, diarrhea, stomach pain, nausea
CONTRAINDICATIONS: EtOH increases active level of drug --> rhabdomyolysis; erythromycin, itraconazole, ketoconazole all contraindicated with lovastatin (Mevacor) especially, but w/ all statins as well --> rhabdomyolysis |
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