右旋泮托拉唑片S-(-)-pantoprazole

Therapeutic category: proton-pump inhibitor
Composition:
Each enteric coated tablet contains S-pantoprazole sodium equivalent to S-pantoprazole…20 mg
Indication: Gastro-esophageal reflux disease, duodenal and gastric ulcer Dose (adults): 20 mg once daily for 4-8 weeks depending upon condition and response
Advantages:
Provides the more potent and cytoprotective component of pantoprazole
Half the racemate dose
Consistent pharmacokinetics
Does not accumulate in poor metabolizers
Offers lesser potential for drug interactions
【药理毒理】
本品为胃壁细胞质子泵抑制剂，在中性和弱酸性条件下相对稳定，在强酸性条件下迅速活化，其pH依赖的活化特性，使其对H+、K+-ATP酶的作用具有更好的选择性。本品能特异性地抑制壁细胞顶端膜构成的分泌性微管和胞浆内的管状泡上的H+、K+-ATP酶，引起该酶不可逆性的抑制，从而有效地抑制胃酸的分泌。由于H+、K+-ATP酶是壁细胞泌酸的最后一个过程，故本品抑酸能力强大。它不仅能非竞争性抑制促胃液素、组胺、胆碱引起的胃酸分泌，而且能抑制不受胆碱或H2受体阻断剂影响的部分基础胃酸分泌。本品与其他药物伍用时，具有药物间相互作用小的优点。本品通过肝细胞内的细胞色素P450酶系的第I系统进行代谢，同时也可以通过第II系统进行代谢。当与其他通过P450酶系代谢的药物伍用时，本品的代谢途径可以通过第II酶系统进行，从而不易发生药物代谢酶系的竞争性作用，减少体内药物间的相互作用。无致突变、致癌和致畸作用。
【药代动力学】
本品具有较高的生物利用度，首次口服时即可以达到70%～80%，达峰时间1小时，有效抑酸达24小时。静脉注射与口服给药的生物利用度比值为1.2。口服40mg时的tmax为2～4小时，Cmax约为2～3g/ml，清除半衰期约为1.1小时。约80%的口服或静注本品的代谢物经尿中排泄，肾功能不全不影响药代动力学，肝功能不全时可延缓清除。t1/2、清除率和表观分布容积与给药剂量无关。
【适应症】
主要用于：
①消化性溃疡出血。
②非甾体类抗炎药引起的急性胃黏膜损伤和应激状态下溃疡大出血的发生；
③全身麻醉或大手术后以及衰弱昏迷患者防止胃酸反流合并吸入性肺炎。
【用法用量】
静脉滴注。一次40mg，每日1～2次，临用前将10ml专用溶剂注入冻干粉小瓶内，将上述溶解后的药液加入0.9%氯化钠注射液100ml中稀释后供静脉滴注，静脉滴注时间要求15～30分钟内滴完。本品溶解和稀释后必须在3小时内用完，禁止用其他溶剂或其他药物溶解和稀释。
【不良反应】
偶见头晕、失眠、嗜睡、恶心、腹泻、便秘、皮疹和肌肉疼痛等症状。大剂量使用时可出现心律不齐、转氨酶升高、肾功能改变、粒细胞降低等。
【禁忌】对本品过敏者禁用；妊娠期与哺乳期妇女禁用。
【注意事项】
本品抑制胃酸分泌的作用强，时间长，故应用本品时不宜同时再服用其他抗酸剂或抑酸剂。为防止抑酸过度，在一般消化性溃疡等病时，不建议大剂量长期应用（卓-艾综合征例外）。肾功能受损者不须调整剂量；肝功能受损者需要酌情减量。治疗胃溃疡时应排除胃癌后才能使用本品，以免延误诊断和治疗。动物实验中，长期大量使用本品后，观察到高胃泌素血症及继发胃ECL-细胞增大和良性肿瘤的发生，这种变化在应用其他抑酸剂及施行胃大部切除术后亦可出现。
【孕妇及哺乳期妇女用药】
妊娠期与哺乳期妇女禁用。
【儿童用药】尚无儿童静脉应用本品的经验。
【老年患者用药】老年人用药剂量无需调整。
【药物相互作用】尚不明确。
【药物过量】
【规格】40mg(以泮托拉唑计)
【贮藏】密闭，遮光保存。
【包装】管制抗生素瓶；1瓶/盒

为比较S-pantoprazole(20 mg 每天一次) vs racemic pantoprazole(40mg 每天一次)治疗胃食管反流疾病(GERD)的疗效和耐受性，研究人员开展了一项多中心、随机、双盲临床试验，入选了369例GERD，并随机给予一片(20mg) S-pantoprazole每天一次(试验组)或40 mg racemic pantoprazole每天一次(参照组)，治疗28天。评估患者GERD症状评分在治疗14和28天时，相对于基线0天减少量，同时观察治疗过程中发生的任何不良反应。在一个研究中心中对入选的54例患者于基线和治疗28天时进行了胃镜检查(GI)。
结果可见，两组在治疗14天时一些症状评分显著减低，包括烧心(P < 0.0001)，反酸(P < 0.0001)，胃胀(P <0.0001)，恶心(P < 0.0001)以及 咽下困难(P <0.001)，且继续治疗至28天后进一步减低。两组间患者治疗14天和28天反酸和胃胀改善的比例也显著不同(反酸P = 0.004 ；胃胀P =0.03)，治疗28天时烧心的改善也不同(P =0.01)，试验组中的改善比例高于参照组，烧心/反酸/胃胀在治疗14天时危险绝对减低约15%，在28天时减低10%；相对危险减低在14天时为26%-33%，28天时减低15%。GI显示两组间食管炎(P= 1)和胃浸蚀(P = 0.27)的治愈率无显著异常。在治疗过程中两组均未报道任何不良反应。
可见，对于GERD 患者，S-pantoprazole (20 mg)较racemic pantoprazole
See Available Brands of Pantoprazole in India
P - Caution when used during pregnancy.
L - Contraindicated in Lactation.
LI - Lab *
Pantoprazole (Sold as Pantotab; Pantopan; Protium; Protonix; Pantozol; Pantor; Pantoloc; Astropan; Controloc; Pantecta; Inipomp; Somac;
Ulcepraz; Pantodac) is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease. Initial treatment is generally of eight weeks' duration, after which another eight week course of treatment may be considered if necessary. It can be used as a maintenance therapy for long term use after initial response is obtained. This medication may affect the results of certain lab tests, such as drug screenings (pantoprazole can cause a false positive for THC). It is recommended you make sure laboratory personnel and your doctor know you are using this drug.
The active ingredient in Protonix (pantoprazole sodium).
Delayed-Release Tablets is a substituted benzimidazole,sodium 5-(difluoromethoxy)-2-[[(3,4-dimethoxy-2-pyridinyl)methyl] sulfinyl]-1 H -benzimidazole sesquihydrate, a compound that inhibits gastric acid secretion.
Pharmacodynamics
Pharmacokinetics
Pantoprazole inhibits H+/K+ ATPase pump function thereby reducing gastric acid secretion. It also has a role in the eradication of H.
pylori.
Absorption
Well absorbed; peak plasma concentrations: Approx 2-2.5 hr after oral dose. Oral bioavailability: Approx 77% with enteric-coated formulation (does not vary after single or multiple doses).
Distribution
Protein-binding: 98%; volume of distribution: 11-24 L.
Metabolism
Hepatic; mainly by cytochrome CYP2C19 and slightly by CYP2D6 and CYP2C0.
Excretion
Via urine (approx 80%) and bile (approx 20%). Elimination half life: approx 1 hour (prolonged in hepatic impairment; in patients with cirrhosis the elimination half life may be 3-10 hours).
Pantoprazole Indications / Pantoprazole Uses
Information Not Available
Pantoprazole Adverse Reactions / Pantoprazole Side EffectsDiarrhoea, dizziness, pruritus, skin rashes, GI tract infections, chest pain, headache, nausea, pain, anxiety, hyperglycaemia; malaise or lassitude; myalgia; oedema; insomnia; hyperlipidaemia; flatulence, abdominal pain, constipation, eructation, dyspepsia, rectal disorder; urinary frequency, UTI; abnormalities in liver function; local site reaction; hypertonia, neck pain, weakness; bronchitis, cough, dyspnoea, pharyngitis, rhinitis, sinusitis, upper respiratory tract infection, flu syndrome.
Precautions
Information Not Available
Special Precautions
Long-term therapy may lead to bacterial overgrowth in the GI tract.
Hepatic impairment; monitor liver function regularly (if enzymes increase, discontinue); pregnancy; not recommended in children <18 yr; long term use may lead to atrophic gastritis.
Other Drug Interactions
Decreased absorption of ketoconazole and itraconazole; may slightly increase digoxin plasma concentration; may reduce plasma concentration of atazanavir, avoid concomitant use; may enhance anticoagulant effect of coumarins; may cause gastric mucosal irritation with alcohol; may increase levels or effects of: bosentan, dapsone, fluoxetine, glimepiride, glipizide, losartan, montelukast, nateglinide, paclitaxel, phenytoin, warfarin, and zafirlukast; may decrease levels or effects of: aminoglutethimide, carbamazepine, phenytoin, and rifampicin.
Other Interactions
Food Interaction
Long term use (>3 yr) may lead to vitamin B12 malabsorption. May decrease oral absorption of iron salts.
Dosage
Oral
Gastro-oesophageal reflux disease
Adult: 20-40 mg once daily in the morning for 4 wk, increased to 8 wk if necessary. Maintenance: 20-40 mg daily, increased to 40 mg each morning if symptoms return.
Hepatic impairment: Doses >40 mg daily have not been studied in hepatically-impaired patients.
Oral
Peptic ulcer
Adult: 40 mg once daily in the morning for 2-4 wk for duodenal ulceration or 4-8 wk for benign gastric ulceration.
Hepatic impairment: Doses >40 mg daily have not been studied in hepatically-impaired patients.
Oral
H.pylori infection
Adult: Triple therapy: 40 mg bid combined with clarithromycin 500 mg bid and either amoxicillin 1 g bid or metronidazole 400 mg bid.
Hepatic impairment: Doses >40 mg daily have not been studied in hepatically-impaired patients.
Oral
Prevention of NSAID-induced ulcers
Adult: 20 mg daily.
Hepatic impairment: Doses >40 mg daily have not been studied in hepatically-impaired patients.
Oral
Zollinger-Ellison syndrome
Adult: Initially 80 mg daily, adjusted to individual requirements. Up to 240 mg daily may be used if needed. Daily doses >80 mg should be given in 2 divided doses.
Hepatic impairment: Doses >40 mg daily have not been studied in hepatically-impaired patients.
Intravenous
Zollinger-Ellison syndrome
Adult: As Na salt: 80 mg once or twice daily. Up to 240 mg daily may be given in divided doses. Convert to oral therapy as soon as possible.
Dose to be given as slow inj or short-term infusion over 2-15 minutes.
Hepatic impairment: May need to reduce dose.
Intravenous
Gastro-oesophageal reflux disease
Adult: As Na salt: 40 mg daily. Convert to oral therapy as soon as possible. Dose to be given as slow inj or short-term infusion over 2-15 minutes.
Hepatic impairment: May need to reduce doses.
Intravenous
Peptic ulcer
Adult: As Na salt: 40 mg daily. Convert to oral therapy as soon as possible. Dose to be given as slow inj or short-term infusion over 2-15 minutes.
Hepatic impairment: May need to reduce doses.
Reconstitution
Reconstitute with 10 ml 0.9% sodium chloride (final concentration 4 mg/ml). Reconstituted solution may be given IV (over 2 minutes) or diluted to 100 ml in glucose 5%, 0.9% sodium chloride, or lactated Ringer's and infused over 15 min.
Incompatibility
Y site incompatibility: midazolam and zinc.
Food(before/after)
Normal release: May be taken with or without food.
Controlled-release: Should be taken on an empty stomach. (Take 1 hr before meals. Swallow whole, do not chew/crush.)
List of Contraindications
Pantoprazole and Pregnancy
Caution when used during pregnancy.
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Pantoprazole and Lactation
Contraindicated in Lactation.
Pantoprazole and Children
Safety and effectiveness in pediatric patients have not been established.
Pantoprazole and Geriatic
In short-term U.S. clinical trials, erosive esophagitis healing rates in the 107 elderly patients (≥ 65 years old) treated with Pantoprazole sodium were similar to those found in patients under the age of 65.
The incidence rates of adverse events and laboratory abnormalities in patients aged 65 years and older were similar to those associated with patients younger than 65 years of age.
Pantoprazole and Other Contraindications
Lactation

Storage
Intravenous
IV (before reconstitution) <25 °C.
Once reconstituted, store <25 °C and use within 12 hours.
Oral
Store tablet at 15-30 °C.
Lab interference
May produce false positive urine screening tests for tetrahydrocan.