| 脳外科でよく使う薬 ||Analgesics/Sedatives || Antiobiotics|| Brain Abscesses and Meningitis|| Anticholinesterases|| Antacids|| Anticoagulants|| Antidiarhheals|| Anti-emetics|| Antiepileptics|| Bronchodilators|| Cardiovascular|| H2-Antagonists|| Laxatives/Stool Softeners|| Muscle Relaxants|| Steroids|| Miscellaneous|| 鎮痛剤及び鎮静剤： Acetaminophen (Tylenol)；Analgesic, antipyretic effects; 弱抗炎症作用 軽い痛みや熱に使用、Hepatic metabolism and renal excretion、Half-life 2 hr 大人； 325-650 mg PO/PR q4-6h、 小児； 10mg/kg PO/PR q4-6h 副作用； rash, drug fever, thrombocytopenia, nephrotoxicity, hepatotoxicity Chloral Hydrate ；沈静作用、肝代謝; renal/bile excretion Onset 30-60min after PO 、大人；1000 - 2000 mg PO/PR q6h 小児；25 - 100 mg/kg/dose PO/PR; may repeat half the dose once if no effect in 1 hour 副作用； GI upset, rash, leukopenia, MS alterations, acute intermittent porphyria, 低血圧, respiratory/myocardial depression, coma Codeine ；摘要は mild/mod pain, antitussive， Onset 15-20 min PO, IM もっと速い; Duration 4-6h 肝代謝(10% to Morphine), renal excretion、Half-life 2.5h PO, 3.5h IM 痛み；adult 15-60mg PO/SC/IM q4h Tylenol#3 1-2 tab PO q4-6h，小児 0.2 - 1 mg/kg PO/SC/IM q4-6h，Antitussive (容量下限) Morphine 10mg IM = codeine 100mg IM 副作用：呼吸抑制, drowsiness, N/V, 便秘, 静注すれば低血圧 Fentanyl (フェンタネスト) ；Opiod agonist 75 - 125 times more potent than morphine 摘要；as adjunct in anesthesia, pain control ( esp 潜在的に血行力学的に不安定な患者に 肝代謝, renal/fecal 排泄、Onset rapid IV, 10-15 min IM、Duration 1hr，Half-life 220 min (短い効果期間に 脂肪や筋に再分布する; 10- 20 ug/kg以上で使われた時 を除く) Sedation/analgesia 1-2 ug/kg as single dose or /hr IV gtt 副作用；呼吸抑制, 遅脈, seizures, ICP上昇の可能性, 骨格筋固縮,便秘, rash, 尿閉 Ibuprofen (ブルフェン, Advil, Nuprin) ；cyclooxygenase とprostaglandin 合成を阻害 摘要； mild/mod pain, as antiinflammatory or occ as antipyretic Hepatic metabolism, renal excretion、Half-life 2hr Analgesic: 200-400 mg q4-6h、Antiinflammatory: 1200-3200 mg/day divided tid-qid 副作用；GI upset, PUD/bleeding, allergic reaction, edema, inc LFT's,ARF Ketorolac Tromethamine (Toradol)；Indicated as NSAID, and analgesic (mild-mod) Hepatic metabolism and renal excretion、Half-life 4-6h 30-60mg IM initially, then 15-30mg IM q6h New PO form availble 30mg tab (inc GI side effects) 副作用；気管支痙攣, GI upset/出血, 肝毒性, 腎毒性, 血小板凝集阻害(薬中止後24-48h 続く) Meperidine (塩酸ペチジン)；麻薬誘導体 6-8 times less potent than morphine 摘要；mod-severe pain, postop shivering, 肝代謝と腎排泄，Half-life 3-4 hr Adult: 50 - 150 mg PO/IM/SC q3-4h; 20-40 mg IV slowly over minutes 10-20 mg IM for postop shivering Ped 0.5-1.5 mg/kg PO/IM/SC q3-4h 副作用；多幸, 眠気, 呼吸抑制, GI upset, 便秘,尿閉,低血圧, seizures, atropine様作用 , 大量でneg inotrope Midazolam (ドルミカム，Versed)；Benzodiazepine with amnesic, 不安解消, 筋弛緩作用 摘要；鎮静．肝代謝と腎排泄．Onset 1-5 min IV, 15 min IM、Duration 1-4 hr IM, 30-60分 IV、Half-life 2-6hr 大人；1-4 mg IM/IV q2-6hr、小児； 0.035-0.1mg/kg/dose 副作用； 呼吸抑制, hypotension, confusion, oversedation, hypersensitivity Benzodiazepine拮抗薬: フルマゼニルFlumazenil 0.2mg IV followed by 0.1mg/min to 1mg(max 5mg total) Morphine ；Opiod agonist 摘要； mod/severe pain, 鎮静, 麻酔の補助薬, 肺浮腫中の血管拡張, MI； sympathetic outflow of "diencephalic fits"も削減する Hepatic metabolism, renal/bile excretion Onset minutes IV/IM, 15-60min IT; Peak 15min IV, 40 min IM Duration 3-5hr IV/IM, 24hr IT、Half-life 2-3hr IM/SC: Adult 5-10mg/70kg q4-6h ,小児 0.1-0.2mg/kg q4-6 IV: Adult 1-5mg q2-4h, Ped 0.1mg/kg q3-4h IT: 0.5-1.0 mg q18-24h 副作用；meperidineに似るがhistamine 放出もある, biliary spasm, ICP上昇の可能性, GI upset, addiction Oxycodone (パビナール,Percocet, Percodan)；合成麻薬 、摘要； mod-severe pain 肝代謝, renal excretion、1-2 tab PO q4-6h、副作用；similar to morphine Percocet (5mg plus 325mg acetaminophen)、Percodan (4.5mg plus 325mg ASA) Propoxyphene (Darvon, Darvocet)；合成麻薬、Mild-mod pain 肝臓で代謝, 腎臓排泄、1-2 tab PO q 4-6h、Adverse effects similar to morphine Darvon (32 and 65mg tab)、Darvocet-N100 (100mg plus 325mg acetominophen) -------------------------------------------------------------------------------- 抗生物質： Acyclovir (Zovirax)； 摘要； HSV I and II, と 帯状疱疹VZV 感染症 腎臓で排泄、 血中半減期: 3.3 hr w/normal renal function もし免疫不全なら； w/ HSV250mg/m2 IV q8 x 7d、 w/ VZV500mg/m2 IV q8 x 7d もし免疫不全でない； w/HSV encephalitis 10 mg/kg IV q8 x 10dw/HSV genital 5 mg/kg IV q8 x 5d 副作用；静脈炎と腎機能障害 Amphotericin B (ファンギゾン,Fungizone)；全身性真菌感染症に適用。胆道から排泄、 5％糖液に配合 全身感染に； start w/ test dose of 1mg IV over 2 hours then dose 0.25-1 mg/kg/day (ped) , 1-1.5 mg/kg/d (adult) 膀胱感染に； place 3-way foley catheter and use 50 mg/1 liter D5W/day as bladder irrigation x 5 days 副作用；nephrotoxicity, anemia, hypokalemia/hypomagnesemia, fever/rigors, GI upset Ampicillin (Omnipen) 効果；gm+ (not penicillinase-産生staph)好気性菌, とgm-(non-betalactamase-産生 H.influenza と 淋菌) 好気性菌, と嫌気性菌(not Bacteroides)、Renal elimination 大人: 500mg - 2 gm PO/IM/IV q4-6h、 小児: 100-200mg/kg/day IV/IM divided q6h 副作用； hypersensitivity and neurotoxicity Cefazolin (セファメジン,Ancef, Kefzol) Active against gm+(not enterococci, S. pneumoniae, streptococci) and gm- aerobes Poor CSF penetration、Renal elimination Adult: 0.5 - 1.5 gm IV/IM q6-8h、 Ped: 50-100 mg/kg/d divided q8h 副作用は ampicillinと同じ Cefotaxime (セフォタックス,Claforan) 効果； gm+(not enterococci or MRSA) と gm-( resistant Enterobacteriaceae と H.influenzaeは含むが P. aeruginosaは除く) aerobes、CSF 移行良好、Renal excretion 大人；1 - 2 gm IV/IM q4-6h 、小児；100-200 mg/kg/d IM/IV divided q6-8h 副作用； similar to other cephalosporins Ceftazidime (Fortaz) 効果；gm+(not enterococci or MRSA) とgm- (特にP. aeruginosa) aerobes と anaerobes(not Bacteroides)、 CSF移行良好、Renal excretion Adult: 0.5 - 2 gm IV/IM q8-12h、Ped: 100-150 mg/kg/d IM/IV divided q8h 副作用； similar to other cephalosporins Ceftriaxone (ロセフィンRocephin)；Same spectrum as Ceftazidime except not P. aeruginosa Also treats Lyme borreliosis、Renal and biliary excretion、Good CSF penetration Adult: 0.5 - 1 gm IV/IM q12-24h、Ped: 50-100 mg/kg/d IV/IM divided q12-24h 副作用；similar to other cephalosporins Ciprofloxacin (シプロキサン、Cipro)； 効果； staphylococci(MRSAを含む)とgm- aerobes (P. aeruginosa not other Pseudomonas類), some streptococci, not anaerobes 使用；resistant 尿路感染症, GI infections, STD's, 骨髄炎, skin/soft tissue 感染 Renal excretion、Poor CNS penetration Adult: 250 - 750 mg PO/IV q12h 副作用； GI upset, HA, restlessness, rash, theophylline elimination reduced Clindamycin (ダラシン、Cleocin)； 効果； gm+ (not enterococci and MRSA) aerobesと most anaerobes (except C. difficile)but not gm- organisms Poor CSF penetration、Hepatic metabolism; renal excretion 大人；600 - 1200 mg/d PO/IV/IM divided q6-8h、小児；25-40 mg/kg/d IV/IM divided q6-8h 副作用； GI upset, diarrhea, rash, leukopenia, thrombocytopenia, eosinophilia Gentamicin (Garamycin) 効果；staph (not streptococci), enterococci (only w/ a penicillin or vancomycin)と多くのgm- aerobes (including Pseudomonas) but no anaerobes Renal excretion、Poor CNS penetration Adult/Ped: 1 - 1.7 mg/kg IV q8h maintenance, preceded by a loading dose of 2 mg/kg IV 腎機能障害では維持量を調節する、Obtain gent levels after 3rd or 4th dose Peak (< 10-12 ug/ml); Trough (< 1-2 ug/ml 副作用；ototoxicity, renal failure Imipenem （チェナム）と Cilastin (Primaxin) 効果；most gm+ とgm- aerobes and anaerobes plus Campylobacter, Yersinia, Nocardia,Mycobacteria, etc., but not enterococci or MRSA or Pseudomonas maltophilia or cepacia Renal metabolism and excretion、Adult: 0.5 - 1 gm IV q6-8h 副作用；rash, GI upset, phlebitis, hypotension, seizure activity Metronidazole (フラジール,Flagyl) 効果；protozoa(ie, トリコモナス, Amebiasis, Giardiasis, Leishmaniasis)とobligate anaerobes Also useful to treat C. difficile associated pseudomembranous colitis Hepatic metabolism-1/3, renal excretion、Excellent CSF penetration Adult: 7.5 mg/kg IV/PO q6h, 2 gm PO single dose for Trichomonas UTI 500 mg PO bid x 10d for Pseudomembranous colitis 副作用；Etoh intolerance, 痙攣, neuropathies, HA, 混迷, GI upset, leukopenia, dark urine Norfloxacin (バクシダール, Noroxin)； Ciprofloxacin と同じ抗菌領域, 摘要；大人の UTI's、Hepatic metabolism and renal excretion、400 mg PO bid 副作用； GI upset, HA, dizziness Oxacillin (Prostaphlin)；Antistaphylococcal activity、Renal excretion after partial metabolism 0.5 - 2 gm IV q4-6h adult、 25 - 35 mg/kg IV q4-6h pediatric 25 mg/kg IV for preop shunt prophylaxis in pediatric cases 1 gm IV for preop shunt prophylaxis in adult cases 副作用；hypersensitivity reactions, GI upset, cytopenias, drug-induced hepatitis Penicillin (Bicillin, Wycillin, Pen-Vee-K)； 効果；gm+ aerobic cocci (streptococci, pneumococci), enterococci (w/aminoglycoside), all anaerobes (B.fragilis 族を除く) 特にActinomyces, non- penicillinase 産生staphylococci, spirochetes, meningo cocci, あるNeisseria種 es, Pasteurella, agents of rat bite fever Renal excretion Penicillin G Adult 0.5 - 1 gm PO q6h , Ped 6.25 - 12.5 mg/kg PO q6h Penicillin V Adult 0.25 - 0.5 gm PO q6h ，Ped 6.25 - 12.5 mg/kg PO q6h， Aqueous Penicillin G (K or Na) Meningitis or Endocarditis 18 - 24 million U/day IM/IV divided q4h Anaerobic Lung/Grp A Strept 8 - 12 million U/day IM/IV divided q4h Procaine Penicillin 300,000 - 4.8 million U/day IM divided q6-24h Benzathine Penicillin 2.4 million U IM single dose or weekly for 3 weeks for syphilis 副作用；過敏反応, 脳症,痙攣, coombs + rxn, 自己免疫, 腎毒性, cytopenias, Procaine rxn, GI upset Rifampin (Rifadin) 効果；Mycobacteria, gm+ (esp staph)とgm- (esp Neisseria species とH. influenzae) 菌 Synergistic w/other antibiotics in treating 異物感染症, endocarditis, legionellosis, 骨髄炎 600 mg/day PO single dose又は divided bid (Adult) 10 - 20 mg/kg/day PO single dose 又は divided bid (Ped) 副作用；肝毒性, アレルギー性と かぜ様症候群, "Red Lobster" syndrome w/overdose Decreases effect of many drugs Ticarcillin （チカルペニン）と Clavulanic Acid (Timentin) 効果；gm+ aerobes (incl staph), most gm- aerobes (incl P. aeruginosa) と anaerobes (incl B. fragilis)、 Renal excretion、Useful empirically w/ mixed infections Adult: 3.1 gm IV q4-6h 副作用； similar to other penicillins Tobramycin (トブラシン,Nebcin) 効果；Staph (not streptococci or pneumococci), enterococci (w/PCN or Vanco), most gm-aerobes (esp P. aeruginosa) but no anaerobes Renal excretion 、Poor CSF penetration 1 - 1.7 mg/kg IV/IM q8h (Adult)、2 - 2.5 mg/kg IV q8h (Ped) Loading dose of 2 mg/kg IV 80 mg IV as preop prophylactic in combination w/Vancomycin when adult patients are allergic to penicillins/cephalosporins 副作用； similar to Gentamicin (see above) 3〜4回投与後に薬容量を測る、頂点 5 - 12 ug/ml 谷 < 1 - 2 ug/ml Trimethoprim （バクタ）と Sulfamethoxazole (シノミン,Bactrim, Septra) 効果； most gm+ とgm- aerobes (some MRSA but not P. aeruginosa), but not anaerobes Useful in UTI's, 呼吸器感染, otitis, Pseudamonas other than aeruginosa, Nocardiosis, and GNR 髄膜炎 肝代謝と腎排泄、Excellent CSF penetration 大人: PO 160mg TMP/800mg SMX q12h IV 4 - 5 mg/kg (based on TMP) q6-12h Ped: PO/IV 4 - 5 mg/kg (based on TMP) q6-12h 副作用；痙攣, 肝毒, mental depression, GI upset, rash, cytopenias, 血清creatinine増加 Vancomycin (Vancocin) 効果；gm+ aerobes, 特にstaph (incl MRSA), 連鎖球菌, enterococci, Diphtheria, C.difficile- による腸炎、 Renal excretion Adult: PO 0.125 - 0.5 gm q6h IV 15 mg/kg q12h or 6.5 - 8 mg/kg q6h Ped: PO 12.5 mg/kg q6h , IV 10 mg/kg q6h Adjust for impaired renal function 副作用；アレルギー反応, 静脈炎, 熱, 耳と腎毒性, neutropenia, "Red Neck "症候群, 低血圧 Zidovudine (レトロビル、AZT) (Retrovir)； 効果； human retroviruses、Good CNS penetration Adult: 200 mg PO q4h、reduce dose w/anemia or granulocytopenia 副作用； anemia, granulocytopenia, HA, myalgia, insomnia, GI symptoms 脳膿瘍と髄膜炎の治療手順 脳膿瘍 副鼻腔炎や先天性心疾患が原因の場合（連鎖球菌）：大量Penicillin又は第3世代Cephalosporin 中耳炎, mastoiditis, or lung abscess (anaerobes and Enterobacteriaceae)に2次的発生； 大量Penicillin とmetronidazole と3rd generation Cephalosporin 術後又は外傷後の2次的な場合(S. aureus, Enterobacteriaceae)； Nafcillin (or Oxacillin) と 3rd generation Cephalosporin 髄膜炎 年令１ヶ月以下(複数菌including grp B or D strept, 町内細菌, Listeria, H. influenzae, meningococci, and pneumococci)の場合； Ampicillin と aminoglycoside (又は 3rd generation Cephalosporin) １ヶ月から３ヶ月児(H. influenzae, pneumococci, meningococci, and grp B streptococci)； Ampicillin と 3rd generation Cephalosporin ３ヶ月以上から１０歳未満(H. influenzae, pneumococci, and meningococci)； 3rd generation Cephalosporin, or cefuroxime, or ampicillin and hloramphenicol 大人； Noncompromised (meningococcal, pneumococci, grp A streptococci)； High dose Penicillin or chloramphenicol or 3rd generation Cephalosporin Compromised (免疫抑制/alcoholism/老人) (above and Enterobacteriaceae, H.influenzae, P. aeruginosa, Listeria)； Ceftazidime と aminoglycoside Add Ampicillin for Listeria 手術後 (S. aureus, P. aeruginosa, Enterobacteriaceae)； Nafcillin (or Oxacillin) and Ceftazidime and aminoglycoside 外傷後： Early (発症３日以内; pneumococci, grp A streptococci)； 多量のPenicillin or Chloramphenicol Late (onset after 3 days; S. aureus, P. aeruginosa, Enterobacteriaceae)； Nafcillin (or Oxacillin) と ceftazidime と aminoglycoside -------------------------------------------------------------------------------- 抗コリン剤Anticholinesterases 一般情報 適用； 重症筋無力症, 非脱分極性筋弛緩剤に拮抗作用, Ileus, bladder atony. 腎臓排泄 Neostigmine (ワゴスチグミン,Prostigmin)；作用開始 4 - 8 min after IV 作用時間 2 - 4 h after IV Nondepolarizing muscle relaxant 拮抗剤； Adult- 0.5 - 2.5 mg slow IV (give 0.6 - 1.2 mg atropine IV before neostigmine) Ped- 0.04 mg/kg/dose Myasthenia gravis: adult: 15 - 50 mg PO tid 、Ped: 2 mg/kg/day PO in 3-4 divided doses Ileus: 0.25 - 1 mg IM/SC q4-6h Pyridostigmine (メスチノン、Mestinon)； 作用開始 2 - 5 min after IV、作用期間2 - 3 h after IV Nondepolarizing muscle relaxant antagonist: 10 - 30 mg IV (preceded by 0.6 - 1.2 mg atropine IV) Myasthenia gravis: 60 - 180 mg PO bid-qid (1500mg/日まで) -OR- sustained-release tablets of: 180 - 450 mg PO qd-bid (adult) 1 - 2 mg/kg PO q3-4h (Ped) -------------------------------------------------------------------------------- 制酸剤 一般情報： -Acts by neutralizing gastric acid and by increasing lower esophageal sphincter tone -Used in treatment of PUD, GER, Stress ulcer prophylaxis -All are best given 30 min - 2 hr postprandially and at hs -All antacids はH2-blockersの吸収を妨害し, sucralfateの効果を妨害するする。 Magnesium/Aluminum-containing (Maalox, Mylanta, Riopan; Al-only: Alternagel, Rolaids) -Mg-containing antacids have osmotic laxative effects -Al-containing antacids are phosphate binders PUD: 5 - 10 ml PO per dose pc and hs Stress ulcer prophylaxis: 15 - 30 ml pNG/PO q1-4h for gastric pH < 4.5 (If pH < 3.5 dose is doubled) 副作用；Mg- 下痢, Mg intoxication in CRF、Al- 便秘, Al intoxication in CRF Alginic acid - containing (Gaviscon) -Forms a floating layer on gastric contents, acting as barrier to GER -Alginic acid is not absorbed、-PUD: 15 - 30 ml PO pc and hs -Stress ulcer prophylaxis: same as in Mg-Al antacids -------------------------------------------------------------------------------- 抗凝固剤Anticoagulants；Aspirin (Ecotrin, Bayer, Bufferin, others) 一般情報： cyclooxygenaseをアセチル化してprostaglandin合成を阻害．結果として； 1) peripheral effect on pain and inflammation 2) decreased hypothalamic "set-point" for antipyretic effect 3) decreased thromboxane in platelets and decreased platelet aggregation for 7-10 d -Indicated in risk reduction in MI, CVA, and TIA -Hepatic metabolism and renal excretion、-Half-life 15 min; salicylic acid 3 hr Dose variable: MI 80 mg PO qd、CVA/TIA 325-1300 mg PO qd 副作用； GI upset, PUD, GI出血, hepatic injury, allergic reactions, prolonged BT 小児には使用しない．ASA と ウイルス疾患（Reye's 症候群）との関係のため Heparin antithrombin III, activated factor II と Xの間の複合体形成促進させる． -Also partial inhibition of XIIa, XIa, IXa, and platelet function 摘要；DVT/PEの予防/治療, 頚動脈手術中のcrescendo TIA's, カテーテル閉塞防止、-Hepatic metabolism and renal excretion -Onset instantaneous after IV、-Half-life 60 min w/ 100 U/kg IV DVT prophylaxis: 5000 U SC q8-12h DVT/PE/TIA therapy: 100 U/kg IV load (5-10,000 U)followed by 800 - 1200 U/hr titrated to maintain PTT 1.5-2 times control Catheter 開存；10 - 100 U IV q8h depending on type/location of catheter, or 5 U/hr art line 副作用；1-33% risk of hemorrhage (esp w/ recent neurotrauma/neurosurgery, 血小板減少症, coag disorder), 血小板減少症と "white-clot" 症候群(血栓性血小板減少症), allergic reaction -Protamine can neutralize heparin by using slow infusion of 1mg per 100 U heparin remaining in patient (est. by 60 min plasma half-life) Warfarin Sodium (Coumadin)；-Inhibits vitamin K-dependent factors II, VII, IX, X in liver -Indicated for prolonged anticoagulation in DVT/PE, AFib, prosthetic heart valves -Hepatic metabolism, bile/renal excretion、-Half-life 36h、-Duration 2-5 d -Initially 10-15mg PO qd for 2-3 days, then reduce to 2.5-10 mg PO qd to achieve steady PTvalues 1.5-1.8 times control -PT reflects previous days dose of warfarin 副作用；出血, teratogenicity, 脂肪の多い組織の皮膚壊死(protein C値減少による； warfarinを使用前に heparin治療をするとこの危険は減少する), leukopenia, 熱 Overdose treatment: Non-lifethreatening - ；Vit K 10-20 mg PO or 5-10 mg IV (< 1mg/min) will reverse warfarin w/in 4-24h; may repeat dose Life-threatening - ；FFP (3 U will return PT to 14-15s) -Many drug and disease state interactions. -------------------------------------------------------------------------------- 下痢止めAntidiarrheals： 治療の前に原因を究明すること。 鼻腔栄養 (High osmotic load), 薬剤性(esp antibiotics), 感染性(viral or C.difficile, Campylobacter, Shigella, Salmonella), 炎症性腸疾患, 過敏性腸,etc. 感染性の下痢は WBC, 卵 や Parasites, 培養, C. difficile 毒素.などの検査をする． 感染性であれば腸運動減少剤は処方しない． 腸運動減少 Diphenoxylate and Atropine (Lomotil) 1 - 2 tabs or 5 - 10 ml of (2.5-5.0 mg dipheoxylate/25- 50 ug atropine) bid - tid 副作用； bloating, abd pain, anticholinergic, constipation Loperamide (ロペミン,Immodium) 2 caps (4mg), then 1 cap (2mg) after each loose stool to a max of 8 caps (16mg)/day 1 cap (2mg) bid-qid if needed chronically、副作用；similar to Lomotil Belladonna alkaloids と Opium (Donnagel-PG, B & O) 30 ml initially, then 15 ml q3h prn 副作用； 便秘, abd cramp, anticholinergic side effects Paregoric (Parepectolin w/kaolin と pectin) 15 - 30 ml after each loose stool up to 8 doses/day 副作用； constipation, abd pain, confusion, allergic reactions -------------------------------------------------------------------------------- その他 Kaolin and Pectin (Kaopectate) - Kaolin absorbs bacteria and toxins, reduces water loss - Pectin stimulates intestinal growth, colonic absorption - 45 - 120 ml after each loose stool up to 8 doses/day、- adverse effect is constipation Bismuth Subsalicylate (Pepto-Bismol)；-unknown mechanism - 2 tsp or tabs q30min - 1h up to 8 doses/day 副作用；便秘, salycilate toxicity, GI bleeding, hemoccult-negative dark stools -------------------------------------------------------------------------------- 制吐剤Antiemetics Promethazine (ピレチア、Phenergan)： 中枢性ムスカリン作用を有する抗ヒスタミン剤；又、前庭刺激を減少させる - Adult: 12.5 - 50 mg PO/PR/IM q4-6h; also 12.5 mg IV q15min titrated to effect - Ped: 0.25-1mg/kg/dose IM/PO/PR tid-qid 副作用； drowsiness, dry mouth, confusion Hydroxyzine (アタラックス、Vistaril)；- 抗ヒスタミン作用。 大人: 50 - 100 mg IM q4-6h、- 小児: 0.5-1 mg/kg/dose 副作用は Phenerganと同じ Prochloperazine (Compazine)； 延髄の chemoreceptor trigger zoneを抑制 - Useful during chemotherapy - Adult: 5 - 10 mg PO/PR/IM/IV q6-8h、- Ped: 0.13 mg/kg/dose IV/IM q6-8h 副作用；急性dystonic 反応様な錐体外路症状 (treated w/ benadryl 50 mg IM/IV), permanent tardive dyskinesia, drowsiness 痙攣閾値を下げるので脊髄造影剤 (esp metrizamide) が使われる時は使用を避ける。 Trimethobenzamide (Tigan)；- Inhibits chemoreceptor zone - 250 mg PO tid-qid or 200 mg PR/IM tid-qid 副作用； parkinson-like symptoms, drowsiness, hypotension, blurred vision -------------------------------------------------------------------------------- 抗テンカン剤 Antiepileptics Carbamazepine (Tegretol)： - Indicated in complex partial seizures, generalized tonic-clonic seizures - 又, 三叉神経痛や他の neuropathic pain syndromesに有効。 - Hepatic metabolism and renal excretion - Induces its own metabolism by inducing liver enzymes、- 血漿半減期: 6.1 +/- 0.7 hr - 大人の量：10 - 20 mg/kg/日 PO (少量より始め週毎に 200 mg/日 ずつ効果があるまで増量)(ある例では 800 - 2400 mg/日必要な事もある) - 小児量：20-30 mg/kg/day PO 副作用；allergic reaction, rash, stimulation of ADH, blurred vision, 酔っ払い気分 - Many drug interactions、- Monitor drug levels: 4 - 12 ug/ml therapeutic range Clonazepam (ランドセン,Clonopin)； - Benzodiazepine derivative 摘要；myoclonic 発作, 局所運動発作の補助薬, second-line to ethosuximide or valproate for absence and akinetic seizures - Hepatic metabolism and renal excretion、 - Plasma half-life: 23 +/- 5 hr 大人：1.5 mg/日PO divided tid 最初に最大量, 3日毎に効果があるまで 0.5 - 1 mgずつ増量 or max 20 mg/日 小児； 最初0.01-0.05 mg/kg/日divided bid-tid , その後3日毎に 0.5 mg/日増量，最大 0.2 mg/kg/日まで 副作用；行動変化, 鎮静,唾液増加, urinary symptoms, cytopenias, rash, hepatotoxicity Benzodiazepine 拮抗剤；Flumazenil 0.2mg IV followed by 0.1mg/分to 1mg (総量max 5mg) Diazepam (セルシン、Valium)；- テンカン重積に適用。- 静注後作用開始 1 - 5 分以内。 - Plasma half-life: 10 - 100 hr - Hepatic oxidation, renal excretion 大人；1 - 2 mg/min IV up to 15 mg for status、小児；0.1-0.3 mg/kg/dose IV up to 5 mg - Must start another antiepileptic drug (eg Dilantin) since effect is short lived 副作用；sedation, respiratory depression, hypotension Benzodiazepine 拮抗薬；Flumazenil 0.2mg IV followed by 0.1mg/分to 1mg (総量max 5mg) Ethosuximide (Zarontin)； 摘要； absence seizures - Hepatic metabolism and renal excretion、- Plasma half-life: 60 hr in adult; 30 hr in peds - Adult: 15 - 30 mg/kg/d PO bid-qid、- Ped: 15 - 40 mg/kg/d PO bid-qid 副作用；rash, SLE-type reactions, GI symptoms, cytopenias, mental confusion - 40 - 100 mg/ml therapeutic range in plasma Lorazepam (ワイパックス、Ativan)； Benzodiazepine 誘導体 摘要；テンカン重積とalcohol withdrawal、Diazepamより効果は長い - Hepatic conjugation and renal excretion、- Plasma half-life: 15 hr mean 重積； 大人；1-4 mg IV up to 6 mg total ，小児 ；0.01-0.02 mg/kg/dose IV up to 0.04 mg/kg/dose 副作用；similar to diazepam Benzodiazepine拮抗薬；Flumazenil 0.2mg IV followed by 0.1mg/分 to 1mg (max 5mg total) Phenobarbital (Luminal) ； 摘要；多くの型のテンカン（重積も含む） 肝代謝と腎排泄、 作用開始； IVは 5 min; 20 - 60 min PO - Plasma half-life: 53 - 118 hr 大人；50 - 100 mg PO/IV/IM bid-tid、重積- 10 mg/kg IV at 50 mg/min up to 20 mg/kg 小児；4 - 6 mg/kg/d IV divided qd-tid、重積 - same as adult - Sedation: 1-3 mg/kg/day IV/PO 副作用；呼吸抑制, airway spasm, 低血圧, 遅脈, GI 症状, rash, Stevens-Johnson 症候群 - Monitor drug levels: 治療域20 - 40 ug/ml Phenytoin (アレビアチン、Dilantin) 摘要；全般性tonic-clonic seizuresの治療と予防, テンカン重積, some partial seizures - Hepatic oxidation and enterohepatic circulation then renal excretion - 95 % bound to plasma proteins、- Plasma half-life: 7 - 42 hr; ave. 22 hr - Phenytoin precipitates in glucose solutions 経口投与量；100 mg tid or 300 mg qhs (steady state 5 - 10 d) 1 gm divided tid over 24 hrs can be used to achieve steady state more rapidly - IV and Status: 15 - 18 mg/kg, not to exceed 50 mg/min to avoid arrythmias; then 300 mg or 5 mg/kg/d maintenance - Ped: Loading dose 20mg/kg IV, then 4-8 mg/kg/day IV/po - Monitor levels: 10 - 20 ug/ml therapeutic range 副作用；GI upset, CNS 毒性, 歯肉肥厚, 多毛症, rash, Stevens-Johnson 症候群, 肝毒性, 心室性不整脈, hypotension - Many drug interactions Paraldehyde (Paraldehyde USP) 摘要；痙攣や禁酒による妄想治療の補助薬, テンカン重積 - Hepatic metabolism to CO2 and H2O, and excreted in the lungs - Plasma half-life: 3.5 - 9.5 hr、- Given through glass syringe or red rubber catheters - Reacts to most IV tubing - Adult: IM 5 - 10 ml、IV 5 ml in 100 ml NS at 1 ml/min PO/PR up to 12ml in 10% solution pNG or 10 - 20 ml as oral retention enema - Ped: IM 0.15ml/kg 、IV 0.1 - 0.15 ml/kg diluted w/ NS、PO/PR 0.3 ml/kg 副作用；混迷,めまい,鎮静,循環虚脱, rash, GI upset, 呼吸抑制, hypotension Primidone (Mysoline) 摘要； tonic-clonic, complex partial, and simple partial epilepsy - Hepatic metabolism (Phenobarbital is a metabolite) and renal excretion - Plasma half-life: Primidone 3 - 24 hr, Phenobarbital 72 - 144 hr, PEMA 24 - 48 hr > 8 yr: 250 mg PO tid-qid、 < 8 yr: 10 - 25 mg/kg/d PO divided tid - Monitor drug levels:Primidone 5 - 10 ug/ml、Phenobarbital 15 - 25 ug/ml、PEMA not established 副作用； sedation, ataxia, GI upset, hyperexcitability, rash, SLE-like syndrome, others. Valproic Acid (Depakene, Depakote) 適当；absence seizures, tonic-clonic, myoclonic seizures; less so for partial seizures 肝代謝とrenal excretion、- Plasma half-life: 14 +/- 3 hr 大人；15 - 45 mg/kg divided bid-qid、小児；15 mg/kg/d divided bid-tid up to 60 mg/kg/d max - Monitor drug levels: 55 - 100 ug/ml therapeutic 副作用；GI upset, alopecia, rash, 鎮静, ataxia, 食欲刺激, 稀にfatal 肝炎, 骨髄抑制 気管支拡張剤Bronchodilators 一般情報： β-adrenergic agonists； 非選択的[epinephrine] ,B2 選択的[metaproterenol, isoetharine, terbutaline, albuterol] B2-agonistsは気管の平滑筋を弛緩させ,粘液排出させ, 肺気管の分泌を抑える。 Epinephrine 抗原によるhistamineとleukotrienes放出を阻害し, histamineによる 細気管支収縮,浮腫、血管拡張に拮抗する． 肝代謝, also lungs and other tissues for epi and isoetharine; renal excretion 副作用；頻脈, 高血圧, 不整脈, angina, 不安, 失見当識, seizures, HA, GI upset, 高血糖, hypokalemia, 尿閉 Epinephrine (Adrenalin)； - Has B1, B2, Alpha effects 摘要； anaphylaxis と acute severe allergic reactions、 - Onset 5 min MDI/Neb, 5 - 10 min SC、 - Duration 1-2h MDI/Neb, 0.75-3h SC 0.4-0.5mg MDI、5mg(5ml 0.1% 液) Neb、0.2-0.5mg SC Metaproterenol (Alupent)；- Not very B2 selective、- Onset 5 min MDI/Neb, 30-45 min PO - Duration 3-5h MDI/Neb, 4h PO 1.3-1.95mg(2-3 回吸入)MDI、15mg(0.3ml 5% in 3ml NS)Neb、20mg PO Isoetharine (Bronkosol)；- Onset 5 min MDI,Neb - Duration 2-4hr MDI,Neb 0.68-1.02mg(2-3 inhalations)MDI、5mg (0.5ml 1% in 3ml NS)Neb Terbutaline (ブリカニール,Brethaire, Bricanyl) - Onset 5min MDI/Neb, 45-60min PO, 5-10 min SC - Duration 3-6h MDI/Neb, 6-8h PO, 2-3h SC 0.4-0.6mg (2-3inhalations)MDI、2mg (2ml)Neb、2.5-5mg PO、0.25mg SC Albuterol (Proventil, Ventolin) - Onset 5-10 min MDI/Neb, 30-45min PO、 - Duration 3-6h MDI/Neb, > 8h PO，0.18-0.27mg(2-3回吸入)MDI、2.5mg in 2-3ml NS Neb、2- 4mg PO Ipratropium Bromide (アトロベント,Atrovent) - Not a Beta blocker; anticholinergic (atropine derivative) vagal efferentの気管収縮効果を阻止 - Hepatic metabolism, renal/fecal/bile excretion、- Onset slow, Peak 45-60min - Half-life 2h - 2-3 puffs (0.04-0.06mg)MDI q6h 、副作用： anticholinergic -------------------------------------------------------------------------------- 心臓血管系薬剤： Adenosine (アデホス、Adenocard) 摘要；paroxyxmal SVT 禁忌；2nd/3rd degree AVB, SSS, AF/AFib, VT/VF - Metabolized by RBC's and vascular endothelial cells、- Serum half-life: < 10 sec - 6mg IV, then 6mg IV, then 12mg IV by rapid injection 副作用；transient AVB, 遅脈, flushing, CP, SOB, lightheadedness, しびれ, 嘔気 Angiotensin Converting Enzyme（ACE) 阻害剤 摘要；antihypertensive, and vasodilation in CHF 副作用；低血圧,頻脈, angina,不整脈,セキ, GI upset, 腎不全, cytopenias, CNS 症状, rash Captopril (カプトリル、Capoten)；- Metabolized by liver, renal excretion - Onset 15 min PO, Peak 0.5-1.5h、- Duration 2-6h、- Half-life < 2h - 12.5-25mg PO bid-tid initially, up to max 150mg tid Lisinopril (ロンゲス,ゼストリル,Prinivil, Zestril)；- Not metabolized, renal excretion - Onset 1h PO, Peak 7h、- Duration 24h、- Half-life 12 hr - 10mg PO qd, up to 20-40mg PO qd Enalapril (レニベース、Vasotec) - Hepatic metabolism to active form, renal/fecal 排泄 - Onset 1h PO/15min IV , Peak 0.5-1.5h PO/1-4h IV、- Duration 24h - Half-life 1.3h, metabolite 35h 2.5-5.0mg PO qd, up to 10-40mg PO qd 1.25mg IV q6h (give over 5min), up to 5mg IV q6h -------------------------------------------------------------------------------- Atropine Sulfate； 摘要；bradycardia、- Hepatic metabolism, renal/fecal/bile excretion - Onset 1-2 min、- Half-life: biphasic 2h, then 12h 大人；0.5-1mg IV push; repeat q5min up to max 2mg、小児；0.01mg/kg to max 0.4mg 副作用；不整脈,頻脈, MI, HA, MS changes,尿閉, 眼球圧上昇, 他のanticholinergic effects Beta 拮抗薬 摘要；MI, 高血圧, arrythmias, hyperthyroidism, migraine, essential tremor 副作用；遅脈, 悪化するCHF, 気管支攣縮, 低血糖, 血管収縮, 心停止or AVB w/Ca blockers, rebound phenomenon w/abrupt withdrawal Propranolol (Inderal) - Nonselective B1 and B2 antagonist、- Hepatic metabolism and renal excretion - Onset immediate IV、- Half-life 2.5h IV; 3-6h PO 0.5-1mg IV up to 0.1mg/kg IV、10-80mg PO bid-qid、80-160mg PO qd extended release Esmolol (Brevibloc) - B1 selective antagonist、- RBC esterase metabolism and renal excretion - Onset immediate、- Half-life 9 min 0.5-1mg/kg IV loading, 50 ug/kg/min infusion up to 300 ug/kg/min titrated to effect Labetolol (Trandate, Normodyne) - Nonselective B1, B2, Alpha-1 antagonist、- Hepatic metabolism/excretion - Onset immediate IV、- Half-life 6-8h 100mg PO bid initially, up to 600mg PO bid max 5 - 20 mg IV over 2 min, repeat q5-10min to max 100mg Metoprolol (ロプレソール、セロケン、Lopressor) B1 selective antagonist、- Hepatic metabolism and renal excretion Onset immediate IV、- Half-life 3-7 hr 1-2mg IV up to 0.2mg/kg max、 100-450mg PO qd or divided bid Atenolol (テノーミン．,Tenormin) - B1 selective antagonist、- Hepatic metabolism and renal excretion、- Half-life 6-9h - 50-100mg PO qd -------------------------------------------------------------------------------- Calcium Channel Blockers - Ca++ antagonists、- Vasodilator, depressor of SA/AV node, negative inotrope - Indicated for hypertension, ischemic heart disease 副作用；arrythmias, hypotension, bradycardia, GI upset, rash, CNS symptoms Diltiazem (ヘルベッサー、Cardizem) 肝代謝, renal/bile excretion、- Half-life 3-9 h、- 30mg PO tid-qid up to 360 mg/d Nifedipine (アダラート、Procardia) diltiazem/verapamilよりnodal/myocardial 抑制効果は弱い。 - More vasodilator effect than other Ca channel blockers - Hepatic metabolism, renal excretion、- Onset 5min SL、- Half-life 2h 10-20 mg PO q4-8h up to max 180 mg/d , 絶食時なら舌下錠あり Verapamil (ワソラン,Calan, Isoptin) - Additional indications are SVT (esp AV node reentry), rapid ventricular response in AF/AFib - Hepatic metabolism, renal excretion、- Onset 2-3min IV - Half-life 110 min IV, 4.5-10 hr PO - SVT: 大人； 0.075-0.15 mg/kg bolus over 2 min (repeat in 10min if no response) Infusion 0.005mg/kg/min AF/AFib HR control 80-120 mg PO tid-qid 小児； 0.1-0.3 mg/kg IV over 2 min - Angina: 80-120 mg PO q6-8h - HTN: 80-120 mg PO tid or 240mg Ext Rel PO qd-bid -------------------------------------------------------------------------------- Clonidine (Catapres, Catapre-TTS) 中枢性α-2 agonist, sympathetic outflowを減少, SVRを減弱, レニン/カテコラミン/aldosterone 分泌阻害 摘要；高血圧, opiate/Etoh/nicotine withdrawal - Hepatic metabolism 50%, renal/fecal excretion、- Half-life 12-16h - Onset 30-60 min after PO, Peak 2-4h PO、- Duration 8h PO - Transdermal patch levels at 2-3d；0.1mg PO bid-tid up to max 2.4mg/d - Apply patch 0.1mg q7d, up to 0.3mg - For Withdrawal, 5 - 17 ug/kg PO divided tid 副作用；低血圧, 遅脈, 急に中止はリバウンド現象, GI upset, 便秘,尿閉, インポ, rash, CNS 症状, glucose intolerance, hypothermia - Paradoxical hypertension w/B-blockers Digoxin (Lanoxin) 摘要； SVT/AF/AFib, と CHF、- Minimal hepatic metabolism, renal excretion - Onset 30-120min PO; 30 min IM; 5-30 min IV、- Half-life 36-48h - Therapeutic level 0.6 - 1.8 ng/ml - Initial dose 0.5mg IV, then 0.125-0.25mg IV q4-6h up to 0.75-1.25mg for effect 維持量； 0.125-0.25mg/d PO/IV 副作用； nearly any arrythmia, GI upset, neurologic effects - Hypokalemia/hypomagnesemia increase dig effect - Acute toxicity, give Digibind 800mg IV Dobutamine (ドブトレックス、Dobutrex)；- B1 > B2 > α-1 agonist - Increases conduction, contractility, vasodilation 摘要；CHF, MR, Right heart failure w/ inc PVR - Hepatic metabolism and renal excretion、- Onset immediate、- Half-life 2 min - 2.5 - 10 ug/kg/min IV gtt 副作用；頻脈, ventricular 不整脈, hypotension secondary to vasodilation Dopamine (イノバン、Intropin) α, B1, and dopaminergic 受容体直接刺激 (DA1-血管拡張, 腎/腸間膜/冠動脈/脳; DA2- inhibits preganglionic NE release), indirect release of NE 摘要；低血圧, and to improve RBF/UO、- Hepatic metabolism and renal excretion - Onset immediate、- Half-life minutes DOSES: For primarily dopaminergic stimulation 0.5-2.0 ug/kg/min For both DA stimulation and B1 action 2-5 ug/kg/min For alpha, beta and DA effects > 10 ug/kg/min 副作用；不整脈,頻脈, hypertension, MI, tachyphylaxis w/in 24 hr, inc PCWP Epinephrine - B1 > B2 > Alpha effects - Indicated in cardiopulmonary arrest, hypotension, severe asthma or allergic reactions - Metabolized in liver, kidney, GI tract, and renally excreted - Onset immediate、- Half-life minutes - DOSES: Primarily B1, B2 effects 1-4 ug/min B1, B2, alpha effects > 4 ug/min 副作用；頻脈, inc myocardial demand, 高血圧, arrythmias, decreased RBF, tissue necrosis Hydralazine (Apresoline) - Direct vasodilation of arterioles > venules, reducing diastolic > systolic BP, decreasing SVR, increasin HR/CO; increase in renal, cerebral, coronary, splanchnic circulations 摘要； chronic hypertension or acute lowering of BP in mild to moderate hypertension - Metabolized in liver, renally excreted、- Onset 10-20 min IV, 20-30 min PO - Half-life 3 hr 25 - 50 mg qid PO; 5mg IV boluses q15min up to 20-40mg, and then 5 - 10 mg IV q6h maintenance 副作用；狭心症の悪化, HA, GI upset, 低血圧, peripheral neuropathy, Lupus-like症候群 Isoproterenol (Isuprel) - Primarily B1 and B2 agonist, increased chronotropy/inotropy, decreased DBP, increased SBP, increased myocardial demand, bronchodilator 摘要；bradycardia, AVB, Pulmonary HTN, bronchospasm - Hepatic metabolism and renal excretion、- Onset immediate、- Half-life < 5 min - 1-10 ug/min (0.05-0.1 ug/kg/min) IV gtt - For bronchospasm 1-2 inhalations of 0.25 - 1% MDI q3-4h 副作用； similar to epinephrine Lidocaine (Xylocaine) - Indicated as local anesthetic and ventricular antiarrythmic (class 1a) - Hepatic metabolism and renal excretion、- Onset immediate IV、- Half-life 100 min - Bolus 1-1.5 mg/kg IV repeated in 20 min; then... 1-4 mg/min IV gtt 副作用；遅脈,低血圧,心筋抑制, CNS toxicity (incl seizures), rash, 浮腫, bronchospasm, anaphylaxis Nitroglycerin 直接静脈拡張作用, decreasing PVR/preload/LVEDP, and decreased myocardial demand, 冠動脈流増加, and causes arteriolar dilation at higher doses - Indicated for MI, CHF, systemic and pulmonary HTN - Hepatic metabolism and renal excretion、- Onset immediate IV/SL; slight delay for PO - Half-life 1-4 min IV; 20 min SL; 4h PO、- Angina: 10-400 ug/min IV; ave. 75-100 ug/min -Hypotension: 10-400 ug/min; arteriolar dilation occurs at > 150 ug/min - Other forms: Transdermal patch 2.5-15mg q24h、Ointment 0.5-2 in q6-12h Sublingual 150/300/400/600 ug SL q5-10 min prn 副作用；tachyphylaxis, hypotension, HA, N/V, increased ICP Norepinephrine (Levophed) - Potent alpha > > B1 effect; no B2 effect、- Indicated in hypotension, cardiogenic shock - Hepatic/renal/GI metabolism and reuptake in nerve terminals; renal excretion - Onset immediate IV、- Half-life minutes - 4 - 10 ug/min IV; maybe higher in sepsis, cardiogenic shock 副作用； decreased RBF, HTN, 組織壊死, HA, angina, 遅脈, 不整脈, MI, stroke, seizures Phenylephrine (ネオシネジン、Neo-Synephrine) - Alpha-1 agonist leading to arterial/venous constriction, increased SVR/PVR - Indicated for hypotension、- Hepatic metabolism and renal excretion 、- Onset immediate IV - Half-life minutes、- 20 - 30 ug/min IV titrate to effect 副作用； HA, HTN, reflex bradycardia, MI, decreased organ blood flow Prazosin (Minipress)： - Alpha-1 拮抗剤で動/静脈拡張を来たす。摘要； HTN, afterload reduction in CHF、 - Hepatic metabolism, fecal 90%/renal 10% excretion、- Onset 2hr PO, Peak 2-4hr - Duration 18-24hr、- Half-life 2-4hr、- Initial dose 1 mg PO bid-tid up to max 20 mg/day 副作用；低血圧, 頻脈, edema, GI upset, CNS symptoms, impotence, blurred vision Procainamide (アミサリン、Procan SR, Procainamide) Class 1a antiarrythmic used for SVT, 心室性不整脈, と AF/AFibの再発予防 - Hepatic metabolism to NAPA (active); renal excretion、- Half-life 3-5h - 100 mg/min to effect or to total dose of 1000mg, followed by a infusion of 2-6 mg/min 副作用； torsades de pointe, junctional tachycardia, 低血圧, GI upset, cytopenias Sodium Nitroprusside (Nipride) - Direct vasodilation of arteries > veins、- Indicated for hypertension, acute LV failure - Nonenzymatic degradation to cyanide, then thiocyanate conversion by liver, then 腎排泄 - Onset immediate、- Half-life minutes; thiocyanate 4 d、- 0.5-10 ug/kg/min titrate to effect 副作用； HA, N/V, 低血圧, 頻脈, ICP上昇, hypoxia (pulm shunting), tachyphylaxis, rebound, qualitative platelet defect - Measure thiocyanate levels qd (< 10mg/100ml) if required longer than 48h - Toxicity can be treated w/amyl nitrite and sodium nitrite, and sodium thiosulfate -------------------------------------------------------------------------------- H2-拮抗剤 基礎と夜間の酸分泌を減少, そして食物と薬で酸分泌刺激 摘要；Peptic Ulcer Disease (PUD), Gastroesophogeal 逆流(GER), ストレス潰瘍の予防 Cimetidine (Tagamet) - Hepatic metabolism, renal excretion、- Half-life 2-3 h、- Duration 4-5 h Stress ulcer 予防：300mg IV q6h PUD: 400mg PO bid x 6-8wk, then 400 mg PO qhs GER: 400mg PO bid 副作用；antiandogenic, confusion, 稀に骨髄抑制, many drug interactions Ranitidine (Zantac) - Hepatic metabolism, renal excretion、- Half-life 2-3h、- Duration 4-12h Stress ulcer prophylaxis: 50mg IV q8h PUD: 150 mg PO bid x 6-8wk, then 150 mg PO qhs GER: 150 mg PO bid 副作用； confusion, rare bone marrow suppression -------------------------------------------------------------------------------- 下剤Laxatives/便秘薬Stool Softeners Bulking Agents - Form gel by swelling that stimulates peristalsis - Indicated for constipation and irritable bowel syndrome 副作用； GI impaction due to poor fluid intake, allergic rash, bloating, flatus - Onset 12-24 hr up to 72hr Methylcellulose (Citrucel)；4-6 gm (40-60ml) PO qd Psyllium (Metamucil)；1 tab or packet (powder) qd-tid -------------------------------------------------------------------------------- 軟化剤Emollients - Surfactant that facilitates stool mixing and softening、- Indicated for constipation 副作用； cramping, skin rash、- Onset 24-48h up to 3-5d Docusate Sodium (Colace) - 50-100mg PO bid -------------------------------------------------------------------------------- Lubricants - Coat fecal contents and decreasing water absorption、- Indicated for constipation - Adverse effects include rectal irritation, lipoid pneumoconiosis if aspirated、- Onset 6-8h Mineral Oil (Fleets Enema Oil Retention)；15-60 ml PO prn、1 enema PR prn Saline Agents - Osmotically active and increase intraluminal volume stimulating peristalsis - Indicated for constipation - Adverse effects include cramping, confusion, Mg toxicity (weak, dizzy, decreased DTR's) - Onset 0.5-3h Magnesium Citrate (Citroma)；200 ml PO prn Magnesium Hydroxide (Milk of Magnesia)；2.4-4.8 (30-60ml) gm PO prn -------------------------------------------------------------------------------- Stimulants よく解らない作用機序；直接神経刺激によるかも, 又はfluid, Na, とglucose 吸収減少 - Indicated for constipation, acute rather than chronic 副作用；cramping, diarrhea, confusion, electrolyte disorders, cardiac complications、 - Onset 6-8hr; castor oil 2-6hr Bisacodyl (テレミンソフト、Dulcolax)；1-3 tabs (5-15mg) PO/PR qod-bid prn Casanthrol (Peri-Colace)；Contains docusate sodium, 軟化剤1-2 capsules or TBSP qd-bid prn -------------------------------------------------------------------------------- 高浸透圧薬Hyperosmotic Agents - Increase luminal contents and stimulate peristalsis、- Indicated for constipation - Adverse effects include cramping, diarrhea, flatulence、- Onset within hours Glycerin ；1 supp PR or 3gm PO prn Lactulose (ラクツローゼ、Cephulac)；hyperammonemiaに摘要、15-60 ml PO until first stool, then on q6-8h basis - Monitor daily ammonia levels -------------------------------------------------------------------------------- 筋弛緩剤： Nondepolarizing Agents postsynaptic cholinergic receptor of the NMJの競合的阻害, MEPの脱分極阻止 摘要；手術、挿管,,機械的呼吸の時の骨格筋弛緩 主な危険は呼吸麻痺で airway controlと mechanical ventilationが必要。 Myasthenia, hypokalemia, respiratory acidosis, metabolic alkalosis, 低体温, aminoglycosides, lidocaine, hypermagnesemia は全てnondepolarizing relaxantsの効果を長引かせる。 - Reversal of NMB - IF partial reversal has occurred (ie 1 of 4 twitches on a nerve stimulator) then full reversal can be achieved with an cholinesterase inhibitor and an anticholinergic agent to prevent the unwanted muscarinic effects like bradycardia and sialorrhea: - Atropine 7-9 ug/kg plus edrophonium 0.5-1.0 mg/kg - Glycopyrrolate 7.5 ug/kg plus neostigmine 40-70 ug/kg Pancuronium (ミオブロック、Pavulon) - Hepatic metabolism 25%, renal excretion 60-80%、- No histamine release - 2+ vagal blockade causing tachycardia、- Half-life 100-120 min、- Time to effect 3-5 min - Intubation dose: 0.07-0.08 mg/kg IV、25-50% q1-2h for maintenance Vecuronium (マスキュラックス、Norcuron) 肝代謝 25%, 腎排泄 < 20%、- No histamine release、- Half-life 70 min - Time to effect 2-3 min - Intubation dose: 0.08-0.10 mg/kg IV、1-2 ug/kg/min IV maintenance Atracurium (Tracrium) - Hoffman degradation (Temp and pH dep); nonspecific ester hydrolysis 長期使用は laudanosine 代謝物の蓄積を来たしseizures 又は CNS 興奮になる． - Mild histamine release、- Half-life 20 min、- Time to effect 2-3 min - Intubation dose: 0.4-0.5 mg/kg IV、5-10 ug/kg/min IV maintenance 脱分極剤Depolarizing Agent Succinylcholine (Anectine) 骨格筋のNMJのpostsynaptic cholinergic receptorを脱分極視,fasciculations を起こしflaccid paralysisにする． - Indicated in tracheal intubation、- Hydrolyzed by plasma pseudocholinesterase - Half-life 90 sec、- Onset 45-60 sec IV; 2-4 min IM、- Duration 4-6 min - Intubation dose: 1-1.5 mg/kg IV、(Infants) 2 mg/kg IM 副作用；大量の細胞からのカリウム放出（特にやけど,外傷、敗血症,脊髄損傷患者）prolonged effect in patients with atypical pseudocholinesterase; dysrythmias, myalgias, increase ICP in patients with HI or IC mass lesions, rash, aspiration, malignant hyperthermia -------------------------------------------------------------------------------- 副腎皮質ホルモンSteroids Glucocorticoids DNA転写, carbohydrate/lipid/protein代謝を制御；抗炎症作用;膜安定化;免疫抑制;血管性 浮腫の減少; mineralocorticoid；抗腫瘍作用 摘要；副腎不全,抗炎症,脳浮腫,免疫抑制,喘息, sarcoidosis, COPD, アレルギー反応, hypercalcemia, ITP, 腫瘍 肝代謝と renal excretion 副作用；cushingoid features, 高血糖,免疫抑制,感染の危険性, Na と液貯留, CHF, hypokalemia, metabolic alkalosis, osteoporosis, 多幸, HA, psychosis, pseudotumor cerebri, MS changes, seizures, 膵炎, 成長鈍化, protein 消耗, 筋萎縮, 創傷治癒不良, 副腎抑制, 血栓塞栓, aseptic femoral head 壊死 - Many drug interactions 薬理学的特長 薬, Glucocorticoid Potency ,Mineralocorticoid Potency, Peak Effect (hr), Plasma half-life (分), 生物学的 半減期(hr), 量(mg), 薬 の順。 Dexamethasone 25 0 1-2 110 -210 36-54 0.75 Dexamethasone Triamcinolone 5 0 varied 200 18-36 4 Triamcinolone Methylprednisolone 5 0.5 1-2 80 -180 18-36 4 Methylprednisolone Prednisolone 4 0.8 1-2 115 -212 18-36 5 Prednisolone Prednisone 4 0.8 1-2 60 18-36 5 Prednisone Cortisol 1 1.0 - - 8-12 20 Cortisol Hydrocortisone 0.8 1.0 1-2 80 -120 8-12 20 Hydrocortisone Cortisone 0.8 1.0 1-2 30 8-12 25 Cortisone -------------------------------------------------------------------------------- 脳浮腫； Dexamethasone 10-20mg IV, then 4-6mg IV/PO q4-6h 急性ストレス w/副腎不全； Hydrocortisone 100mg IV q8h; taper when stress period over 急性脊髄損傷； Methylprednisolone 30mg/kg IV bolus over 15min, followed by continuous gtt at 5.4mg/kg/hr x 23hr; 損傷後8時間以内に投与されねばならない -------------------------------------------------------------------------------- Mineralocorticoids 遠位細尿管での Naの再吸収とKとHイオンの排泄----Na, K, H homeostasisの制御 摘要；脊髄損傷患者の様な重症起立性低血圧,原発性副腎不全, hypoaldosteronism - Hepatic metabolism and renal/breast milk excretion 副作用；Na/H2O 貯留, HTN,浮腫,心不全,体重増加, hyponatremia, HA, MS changes, paresthesias, metabolic alkalosis, arrythmias Fludrocortisone acetate (フロリネフ、Florinef) - Peak 1.5 hr、- Plasma half-life 30 min、- Biologic half-life 18-36 hr - 0.05 - 0.2 mg/day PO divided bid ------------------------------------------------------------------- その他 Acetazolamide (Diamox) Carbonic anhydrase 阻害剤 （腎細尿管で水素とbicarbonate イオンの生成減少）, Na, K, H20, HCO3の アルカリ性利尿を来たす。 摘要；metabolic alkalosis, edematous states, Pseudotumor Cerebri, altitude sickness - No metabolism, renal excretion、- Half-life 5hr - Metabolic alkalosis Adult 250mg IV bid-qid、 Ped 8-30 mg/kg/day Altitude sickness 登る前に250 mg qd-qid 24-48hr, then for > 48h to control symptoms 副作用；malaise, anorexia, HA, weakness, しびれ, GI upset, hypokalemia, 代謝性acidosis Acetylcysteine (Mucomyst) - Indicated as mucolytic agent, and in acetaminophen overdose - Hepatic metabolism, unknown excretion、- Mucolytic: 3-5ml 20% solution Neb q2-3hr - Must give in conjunction w/ bronchodilator 副作用； bronchospasm, rhinorrhea, N/V, drowsiness, rash, fever Chlorpromazine (ウィンタミン、Thorazine) - Blocks DA receptors in forebrain and basal ganglia 摘要；diencephalic fits, hiccups, nausea/vomiting - Hepatic metabolism and renal/hepatic excretion、- Half-life 30hr; metabolites months - N/V: 100-200 mg PO/IM q4-6h; 50-100 mg PR q6-8h - Hiccup:25-50 mg PO/IM q4-6h - Diencephalic fits: 50-100 mg IM q4-6h 副作用；鎮静, 錐体外路反応, anticholinergic 効果, 起立性低血圧, neuroleptic malignant syndrome, tardive dyskinesia Desmopressin Acetate (dDAVP) 合成 ADH類似品、 摘要；neurogenic diabetes insipidus - Tissue metabolism、- Half-life 8 min fast-phase; 75 min slow-phase - Duration 8-20h intranasal; 12-24h IV 大人；0.1-0.4 ml (10-40 ug) intranasally qd-bid、2-4 ug (0.5-1.0 ml) IV/SC bid Ped: 0.05-0.1 ml (5-10 ug) intranasally qd-tid 副作用；HA, seizure, 水中毒, labile BP, GI upset, oliguria, hyponatremia, 過敏症 - Potentiates antidiuretic action: carbamazepine, Chlorpropamide, clofibrate - Decrease antidiuretic action: demeclocycline, lithium, epinephrine, norepinephrine, heparin,alcohol Demeclocycline (Declomycin) Tetracycline誘導体、 摘要； chronic management of SIADH No metabolism, 腎排泄、- Half-life 10-17h、- 150-300mg PO q6h (1hr ac or 2hr pc) 副作用；光線過敏, rash, vertigo, discolored nails/teeth, GI upset, 舌炎, 会陰部感染, 心外膜炎, 腎毒性, 肝毒性, neutropenia, 貧血, 血小板減少症, nephrogenic DI Dextran 40 低分子． - Acts as volume expander, anticoagulant, antiplatelet, and promotes peripheral blood flow by inhibiting RBC aggregation and sludging in microcirculation (coats endothelial wall) - No metabolism, renal filtration if < 55,000 daltons、- Onset immediate - Half-life 2/3 eliminated w/in 12hr、 - Prophylaxis of thromboembolism or antiplatelet effect: Continuous IV infusion of Dextran 40 at 30-50 ml/hr 副作用； antigenicity, 腎不全, interference with crossmatching blood Furosemide (Lasix) - Inhibits absorption of Na and Cl in ascending loop of Henle and in proximal/distal tubules - Indicated as a diuretic for HTN, pulmonary edema, edematous states, acute oliguria - Hepatic metabolism, renal/biliary excretion、- Half-life 0.5-1.5hr - Diuretic: adult 10-40mg IV/IM; 20-80 mg PO q6-8h ped 1.0mg/kg IV increased by 1mg/kg q2hr prn、2.0mg/kg PO inc by 1-2mg/kg q6-8h - Antihypertensive: 10-80mg IV/IMup to 100-200mg IV prn、40mg PO bid 副作用； hyponatremia, hypokalemia, hypovolemia, hypomagnesemia, prerenal azotemia, metabolic alkalosis, glucose intolerance Magnesium Sulfate - Indicated in hypomagnesemia、- No metabolism, renal excretion - Duration ；IV immediate onset lasting 30 min、IM peaks 60 min lasting 3-4h - 1mEq = 12 mg elemental Mg - MgSO4 (1gm = 8.12mEq Mg = 98mg Mg) 10-50% solutions - HypoMg seizures/arrythmias: 1-2gm IV over 15 min, then 1-2gm IV q4-6h - Mild hypoMg: 1gm IV/IM q6h x 3-5d plus excess losses - Severe hypoMg: 5gm IV over 4h, then 1gm IV q4-6h x 3-5d plus excess losses - RDA: 300-350mg/d 副作用；血管拡張, 低血圧, heart block, ECG変化, 呼吸抑制, CNS 抑制, マヒ, 低体温,下痢, hypocalcemia - Overdose treated w/ IV Ca 5-10 mEq over 5 min - Serum Mg levels: normal 1.5 - 2.4 mEq/l anticonvulsant 2.5-7.5 mEq/l Dec DTR/BP 7-10 mEq/l resp paralysis 12-15 mEq/l cardiac arrest > 15 mEq/l Mannitol (Osmitrol) - Increases plasma osmolality creating an osmotic diuresis; may act as rheologic agent, and as a free- radical scavenger - Indications include reducing cerebral edema and ICP - Slight hepatic metabolism, renal excretion、- Half-life 100 min - Onset diuresis in 1-3 hr, tissue effect within 15 min、- Duration 3-8 hr ICP reduction - Adult and Ped: 0.25 - 2.0 gm/kg IV (20% solution) q4-6h 副作用；hypernatremia, hypervolemia, ARF 脱水, hypokalemia, 熱, MS changes, CP,痙攣 - Hold mannitol if serum osmolality is > 320 Metoclopramide (プリンペランReglan) 下部食道括約筋圧,食道酸clearanceを上昇させるDopamine強調薬； 胃停滞と蠕動を改善する．嘔吐中枢のchemoreceptor trigger zone 閾値を上げる - Indicated in GER, delayed gastric emptying, peristaltic stimulant, antiemetic - Hepatic metabolism and renal excretion、- Half-life 4-6h、- Duration 1-2h - GER: 10-20mg PO 30 min ac and qhs 胃内容停滞； 10 mg PO 30 min ac and qhs; IV q6h 蠕動促進に； 10-20 mg IV during NDT/FT placement 制吐作用； 1-2mg/kg IV 30 min prior to chemo, repeat q2-4h 副作用；錐体外路効果(treated with benadryl 50mgIV/IM), drowsiness, fatigue Naloxone (ナロキソン、Narcan) - Opiod receptor antagonist 摘要； analgesia, 呼吸抑制, 鎮静, pruritis,尿閉など麻薬の副作用に拮抗 - Hepatic metabolism and renal excretion、- Onset 2-3min IV 、- Half-life 60 min - Duration 30-45 min - Reverse postop narcosis: 1-2 ug/kg IV q5min to desired effect (usually 0.2-0.3mg) - Suspected narcotic OD: 0.4-2.0mg IV initially, up to max of 10mg; can be given IM 副作用；HTN, 不整脈, 肺浮腫, 急に注射は心停止; 中毒者は禁断症状 Nimodipine (Nimotop) - Ca++ channel antagonist もっと脳選択性がある以外他のCa channel blockersと同じ - Indicated for cerebral vasospasm prophylaxis - Has been demonstrated to improve outcome after SAH-induced delayed ischemia - Adult: 60mg PO/NG q 4h. x 21 days 副作用； 他のCa channel antagonistsと同じ； 低血圧症では長期使用禁止 Pentobarbital (Nembutal) - Barbiturate indicated for coma induction as means to control elevated ICP - Hepatic metabolism and renal/fecal excretion、- Onset immediate IV、- Duration 15-50 hr - Half-life variable - Pentobarbital Coma for ICP Control: Loading dose 10mg/kg IV (rate < or = 50 mg/min) then 5 mg/kg/hr IV x 3 hrs, then 維持量 1 - 3 mg/kg/hr IV (use bedside EEG monitoring or serum levels (range 25-40 ug/ml);目標は EEG burst suppression patternが出るまで 副作用；CNS depression, hypoventilation, hypotension, bradycardia, N/V, 便秘 Phosphorus (Neutra-Phos, K-Phos, Potassium or Sodium Phosphate) - Indicated for phosphorus depletion and hypophosphatemia - No metabolism; renal and some GI excretion、- RDA: 800 mg or 26 mmol - 31 mg phosphorus = 1 mmol、- Normal serum level = 3-4.5 mg/dl adult; 4-7 mg/dl ped - Neutra-Phos:250mg (8mmol), 7mEq K, 7mEq Na (PO) Potassium Phosphate: 3mmol PO4, 4.4 mEq K per ml (IV) Sodium Phosphate: 3mmol PO4, 4 mEq Na per ml (IV) - PO4 depletion: recent 0.6mg (0.02mmol/l)/kg/hr、chronic 0.9mg (0.03mmol/l)/kg/hr 維持；250-2000 mg/日 PO divided q6h、10-50 mmol/l/日(310 - 465 mg phosphorus) 副作用；下痢, N/V, abd pain, hyperkalemia, hypocalcemia and Ca precipitation, 腎障害 Rally Pack 急性の病気又は栄養失調（例えばアル中）の危険にある患者に注入 - Thiamine 100 mg IV q day x 3d、- MVI 1 amp IV q day x 3d、- Folate 1 mg IV q day x 3d - Vit C 500 mg PO/NG qd x 3d、- B12 100 mcg IM x 1 dose Sodium Bicarbonate - Indicated in metabolic acidosis、- No metabolism; renal/pulmonary excretion - Half-life indeterminate、- Normal level 22-27 mEq/l、- Usually given for blood pH < 7.2 緊急replacement；最初1.0 mEq/kg IV, followed by 0.5 mEq/kg IV while monitoring pH 緊急でない場合；2-5 mEq/kg IV over 4-8 hr 副作用；metabolic alkalosis, 浮腫, tetany from hypocalcemia, hyperosmolality, hypokalemia, 筋痙攣 Sucralfate (アルサルミン、Carafate) - Indicated for treatment of PUD or GI stress prophylaxis - Not significantly absorbed from GI tract、- Adult: 1 gm. PO/NG q4h 副作用； constipation, mild GI upset Theophylline/Aminophylline phosphodiesterase阻害剤；cAMP 値を上げる； adenosine receptorsに拮抗；細胞内Caを増加； increase sensitivity of medullary CO2 centers; improves diaphragmatic function; relaxes bronchial smooth muscle; increases myocard ial contactility/rate; 胃分泌増加; 腎 salt/water 排泄増加; reduces seizure threshold and brain blood flow; antiinflammatory 摘要；bronchospasm、- Hepatic metabolism and renal excretion - Therapeutic serum level: 10-20 ug/ml - Half-life: 7-9h adults; 4-5h smokers; 3-5h ped; 20-30h premies; Decreased clearance in CHF, liver dysfunction, alcoholism, pulmonary edema, COPD - Theophylline: Loading dose- 5-6 mg/kg PO; 1mg/kg to increase serum level by 2 ug/ml Maintenance- 3mg/kg PO q6h (adult nonsmokers) 4mg/kg PO q6h (adult smokers)、2mg/kg PO q8h (age > 60 yr) 2mg/kg PO q12h (liver/heart failure) - Aminophylline: Loading dose- 5-6 mg/kg IV over 20 min; 1 mg/kg to increase blood level by 2 ug/ml Maintenance- 0.5 mg/kg/hr IV gtt (adult nonsmokers) 0.8 mg/kg/hr IV gtt (adult smokers)、0.3 mg/kg/hr IV gtt (age > 60 yr) 0.2 mg/kg/hr IV gtt (liver/heart failure) 副作用；いらいら, 不穏, HA, seizures, depression, 頻脈, 低血圧,不整脈, GI upset, 下痢, reflux, GI bleeding, fever, rash, urinary retention, hyperglycemia - Many drug interactions Thiopental (ラボナール、Pentothal Sodium) - Barbiturate indicated in general anesthesia, seizures, increased ICP、- Hepatic metabolism - Onset < 1 min IV、- Duration 20-30 min after single dose、- Half-life 3-8h - Induction: 3-4 mg/kg IV (adult)、2-3 mg/kg IV (ped/elderly) - Seizures: 75-125 mg IV (adult) 副作用； 逆行性健忘,低血圧,頻脈, myocardial depression, arrythmias,呼吸抑制, apnea, laryngospasm, bronchospasm, pain/swelling/ulceration/vasospasm/gangrene local effects if tissue infiltrated,allergic reactions, shivering Vasopressin (Pitressin) - Antidiuretic, antihemorrhagic, vasopressor, peristaltic stimulant 摘要；neurogenic diabetes insipidus, 食道静脈瘤出血, postop abdominal distension - Hepatic/renal metabolism and renal excretion、- Half-life 10-20 min - Duration 2-8h IM/SC aqueous vasopressin - DI: Adult 5-10 U IM/SC bid-qid、Ped 2.5-10 U IM/SC bid-qid - Postop abd distention: 5-10 U IM initially, then q3-4h prn - Upper GI bleeding: 0.2-0.4 U/min IV 副作用：CNS 症状, angina, vasospasm, HTN, arrythmias, skin necrosis, hypersensitivity, GI upset, water intoxication, hyponatremia, 気管支狭窄 |
