Absorption, Distribution and Excretion
Rapidly absorbed following both intramuscular and subcutaneous injection. Initial blood levels following parenteral administration are high but transient. Oral absorption in fasting, healthy humans is only about 15-30% as it is very susceptible to acid-catalyzed hydrolysis.
Penicillin G is eliminated by the kidneys. Nonrenal clearance includes hepatic metabolism and, to a lesser extent, biliary excretion.
0.53–0.67 L/kg in adults with normal renal function
560ml/min in healthy humans
...WIDELY DISTRIBUTED THROUGHOUT BODY... ITS APPARENT VOL OF DISTRIBUTION IS IN ABOUT 50% OF TOTAL BODY WATER. MORE THAN 90%...IN BLOOD IS IN PLASMA & LESS THAN 10% IS IN ERYTHROCYTES; APPROX 65% IS REVERSIBLY BOUND TO PLASMA ALBUMIN. LOW CONCN OF PROTEIN...LOW DEGREE OF BINDING...DRUG EFFICACY.
SIGNIFICANT AMT APPEAR IN LIVER, BILE, KIDNEY, SEMEN, LYMPH, & INTESTINE. ... PENICILLIN DOES NOT READILY ENTER CSF WHEN MENINGES ARE NORMAL.
ORAL DOSES OF 500 MG POTASSIUM PENICILLIN G TO HUMAN SUBJECTS RESULT IN URINARY CONCN OF 600 UG/ML, FOR 2 HR, & 300 UG/ML, FOR 4 HR AFTER DOSING. ... INEFFICIENT PLACENTAL TRANSFER IS CONSISTENT WITH LOW LIPID SOLUBILITY & LOW IONIZATION CONSTANT OF PENICILLIN G & THERE IS NO EVIDENCE OF PLACENTAL TRANSPORT.
...RAPIDLY ELIMINATED FROM BODY, MAINLY BY KIDNEY BUT IN SMALL PART IN BILE & BY OTHER CHANNELS. ... CLEARANCE VALUES ARE CONSIDERABLY LOWER IN NEONATES & INFANTS, BECAUSE OF INCOMPLETE DEVELOPMENT OF RENAL FUNCTION...
For more Absorption, Distribution and Excretion (Complete) data for PENICILLIN G (21 total), please visit the HSDB record page.

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Metabolism / Metabolites
About 16-30% of an intramuscular dose is metabolized to penicilloic acid, an inactive metabolite. Small amounts of 6-aminopenicillanic acid have been recovered in the urine of patients on penicillin G. A small percentage of the drug appears to be hydroxylated into one or more active metabolites, which are also excreted via urine.
Approx 16-30% of an IM dose of penicillin G sodium is metabolized to penicilloic acid which is microbiologically inactive. Small amt of 6-aminopenicillanic acid (6-APA) have also been found in the urine of patients receiving penicillin G. In addition, the drug appears to be hydroxylated to a small extent to one or more microbiologically active metabolites which are also excreted in urine.

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Biological Half-Life
In adults with normal renal function is reportedly 0.4–0.9 hours
ELIMINATION HALF-LIFE IS ABOUT 30 MIN IN NORMAL ADULTS.
PENICILLIN HALF-LIFE IN HUMAN SERUM INCR FROM ABOUT 25 MIN IN YOUNG ADULTS TO 2 HR IN ELDERLY SUBJECTS & IS ALSO MARKEDLY INCR BY DRUGS WHICH ARE ACTIVELY SECRETED BY KIDNEY TUBULES. /PENICILLIN/
The serum half-life of penicillin G in adults with normal renal function is reportedly 0.4-0.9 hr.
The serum half-life of penicillin G in neonates varies inversely with age and appears to be independent of birthweight. The serum half-life of the drug is reportedly 3.2-3.4 hr in neonates 6 days of age or younger, 1.2-2.2 hr in neonates 7-13 days of age, and 0.9-1.9 hr in neonates 14 days of age or older.

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Limited information indicates that penicillin G produces low levels in milk that are not expected to cause adverse effects in breastfed infants. Occasionally disruption of the infant's gastrointestinal flora, resulting in diarrhea or thrush have been reported with penicillins, but these effects have not been adequately evaluated. Penicillin G is acceptable in nursing mothers.
◉ Effects in Breastfed Infants
A breastfed 1-month-old infant with congenital syphilis developed a Herxheimer reaction 6 hours after its mother received 2.4 million units of benzathine penicillin G intramuscularly. However, the baby had also received 10 units of penicillin G at about the same time as the mother's injection. The reaction was possibly caused by penicillin in breastmilk.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.

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Protein Binding
Bind to serum proteins (45-68%), mainly albumin.

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Interactions
MARKED POTENTIATION OF HYPOPROTHROMBINEMIC EFFECT OF WARFARIN BY LARGE DOSES OF PARENTERAL PENICILLIN G DESCRIBED IN 49-YR-OLD MALE. PENICILLIN G CAUSED WARFARIN PROTEIN BINDING DISPLACEMENT INTERACTION.
Penicillins are generally inactivated in the presence of heat, alkaline or acid pH, oxidizing agents, alcohols, glycols, and metal ions such as copper, mercury, or zinc. In currently available penicillins, cleavage at any point in the penicillin nucleus, including the beta-lactam ring, results in complete loss of antibacterial activity. The major cause of inactivation of penicillins is hydrolysis of the beta-lactam ring. The course of hydrolysis and nature of the degradation products can vary and are generally influenced by pH. /Penicillins/
Penicillin G is potentially physically and/or chemically incompatible with some drugs, including aminoglycosides and tetracyclines, but the compatibility depends on several factors (eg, concn of the drugs, specific diluents used, resulting pH, temp).
Penicillins are generally inactivated in the presence of heat, alkaline or acid pH, oxidizing agents, alcohols, glycols, and metal ions such as copper, mercury, or zinc. In currently available penicillins, cleavage at any point in the penicillin nucleus, including the beta-lactam ring, results in complete loss of antibacterial activity. The major cause of inactivation of penicillins is hydrolysis of the beta-lactam ring. The course of hydrolysis and nature of the degradation products can vary and are generally influenced by pH. /Penicillins/
For more Interactions (Complete) data for PENICILLIN G (18 total), please visit the HSDB record page.

Therapeutic Uses
Convulsants; GABA Modulators; Penicillins
GINGIVOSTOMATITIS, PULMONARY INFECTIONS, & GENITAL DISEASE PRODUCED BY SYNERGISTIC ACTION OF FUSOBACTERIUM NUCLEATUM (FUSIFORM) & SPIROCHETES PRESENT IN RESPIRATORY TRACT ARE READILY TREATABLE WITH PENICILLIN. /PENICILLIN/
TWO MICROORGANISMS RESPONSIBLE FOR.../RAT-BITE FEVER/ ARE SENSITIVE TO PENICILLIN G. ...DRUG OF CHOICE IN MGMNT OF INFECTIONS DUE TO LIST MONOCYTOGENES... ONLY SPECIES OF PASTEURELLA HIGHLY SUSCEPTIBLE TO PENICILLIN IS PAST MULTOCIDA. ... CAUSATIVE AGENT OF /ERYSIPELOID/...IS SENSITIVE TO PENICILLIN.
PENICILLIN G THERAPY OF SYPHILIS IS ALMOST IDEALLY SAFE, INEXPENSIVE, & HIGHLY EFFECTIVE. ...AGENT OF CHOICE FOR TREATMENT OF ALL CLINICAL FORMS OF ACTINOMYCOSIS...ANTHRAX...GAS GANGRENE...
For more Therapeutic Uses (Complete) data for PENICILLIN G (35 total), please visit the HSDB record page.

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Drug Warnings
WHEN MASSIVE DOSES OF PENICILLIN G SODIUM ARE USED, CONSIDERABLE SODIUM LOAD IS INTRODUCED, WHICH EXPANDS EXTRACELLULAR SPACE & MAY CAUSE EDEMA IN PT WITH HEART FAILURE. /PENICILLIN G SODIUM/
ALLERGIES CAN OCCUR TO PROCAINE COMPONENT, BUT OTHER TOXIC EFFECTS OF PROCAINE ARE VERY RARE. /PROCAINE/
ANURIA INCR HALF-LIFE OF PENICILLIN G FROM NORMAL VALUE OF 1/2 HR TO ABOUT 10 HR.
ALTHOUGH PENICILLIN G PREPN FOR INHALATION THERAPY & FOR TOPICAL APPLICATION TO SKIN & MUCOUS MEMBRANES ARE STILL AVAIL, THEIR USE IS NOT RECOMMENDED BECAUSE PROOF THAT THEY ARE ADEQUATELY EFFECTIVE IS LACKING, & BECAUSE THEY PRODUCE HIGH INCIDENCE OF HYPERSENSITIZATION.
For more Drug Warnings (Complete) data for PENICILLIN G (23 total), please visit the HSDB record page.

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Pharmacodynamics
Penicillin G is a penicillin beta-lactam antibiotic used in the treatment of bacterial infections caused by susceptible, usually gram-positive, organisms. The name "penicillin" can either refer to several variants of penicillin available, or to the group of antibiotics derived from the penicillins. Penicillin G has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. The bactericidal activity of penicillin G results from the inhibition of cell wall synthesis and is mediated through penicillin G binding to penicillin binding proteins (PBPs). Penicillin G is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.

C16H18N2O4S

334.4

334.098

61-33-6

Penicillin G potassium;113-98-4;Penicillin G sodium salt;69-57-8;Streptomycin;57-92-1;Penicillin G procaine hydrate;6130-64-9;Penicillin G benzathine;1538-09-6;Penicillin G benzathine tetrahydrate;41372-02-5;Penicillin G-d7 potassium;352323-25-2

5904

AMORPHOUS WHITE POWDER

1.4±0.1 g/cm3

663.3±55.0 °C at 760 mmHg

214-217 °C
214 - 217 °C

355.0±31.5 °C

0.0±2.1 mmHg at 25°C

1.655

1.67

112.01

2

5

4

23

530

3

CC1([C@@H](N2C([C@@H](NC(CC3=CC=CC=C3)=O)[C@H]2S1)=O)C(O)=O)C

JGSARLDLIJGVTE-MBNYWOFBSA-N

InChI=1S/C16H18N2O4S/c1-16(2)12(15(21)22)18-13(20)11(14(18)23-16)17-10(19)8-9-6-4-3-5-7-9/h3-7,11-12,14H,8H2,1-2H3,(H,17,19)(H,21,22)/t11-,12+,14-/m1/s1

(2S,5R,6R)-3,3-dimethyl-7-oxo-6-[(2-phenylacetyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid

Galofak CilopenBenzylpenicillin Pradupen

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。