Lithium appears as a soft silvery metal that is normally grayish white due to oxide formation. Spontaneous ignition is likely if heated to melting point.
颜色/状态：
Soft silvery-white metal
气味：
ODORLESS
溶解度：
Reacts with water
蒸汽压力：
7.90X10-11 Pa (5.92X10-13 mm Hg) at 400 K (127 °C); 0.000489 Pa (3.67X10-6 mm Hg) at 600 K (327 °C); 1.08 Pa (0.00810 mm Hg) at 800 K (524 °C); 109 Pa (0.818 mm Hg) at 1000 K (727 °C)
稳定性/保质期：
Decomposes in water
自燃温度：
179 °C
腐蚀性：
LIQUID METAL IS CORROSIVE, ATTACKING GLASS OR PORCELAIN AT A TEMPERATURE OF ABOUT 200 °C
IDENTIFICATION AND USE: Elemental lithium is a silver white metal; body centered cubic structure it becomes yellowish on exposure to moist air and it reacts with water. It is soluble in liquid ammonia forming a blue solution. It is used in the manufacture of catalysts for polyolefin plastics; in fuels for aircraft and missiles.It is used in metallurgy, as a degasifier, deoxidizer, desulfurizer; as a grain refiner in non-ferrous metals. Chemical intermediate for butyllithium polymerization catalyst; in alloys with aluminum or magnesium for aerospace uses. It is used in the production of tritium, reducing and hydrogenating agents, alloy hardeners, pharmaceuticals and Grignard reagents. Scavenger and degassifier for stainless and mild steels in molten state, modular iron, soaps and greases, deoxidizer in copper and copper alloys, heat-transfer liquid, storage batteries (with sulfur, selenium, tellurium, and chlorine). Rocket propellants, vitamin A synthesis, silver solders, underwater bouyancy devices, nuclear reactor coolent. HUMAN EXPOSURE AND TOXICITY: Elemental lithium causes severe eye and skin burns. Industrial exposures to lithium may occur during extraction of lithium from its ores, preparation of various lithium compounds, welding, brazing, enameling, and from the use of lithium hydrides. ANIMAL STUDIES: No animal studies could be located.
Liver test abnormalities have been reported to occur in a small proportion of patients on long term therapy with lithium. These abnormalities are usually asymptomatic and transient, reversing even with continuation of medication. Instances of more marked elevations in serum aminotransferases have been reported in patients taking overdoses of lithium, but the other metabolic and systemic effects of lithium overdose generally overshadow hepatic adverse effects. Lithium has not been associated with instances of clinically apparent acute liver injury with jaundice.
◉ Summary of Use during Lactation:Lithium excretion into breastmilk and concentrations in infant serum are highly variable. Although lithium appears on some lists of drugs contraindicated during breastfeeding, many sources do not consider it an absolute contraindication in healthy-full-term infants, especially in infants over 2 months of age and during lithium monotherapy. Numerous reports exist of infants who were breastfed during maternal lithium therapy without any signs of toxicity or developmental problems. Most were breastfed from birth and some continued to nurse for up to 1 year of maternal lithium therapy. Some reports suggest that lithium in milk can adversely affect the infant acutely when its elimination is impaired, as in dehydration or in newborn or premature infants. Neonates may also have transplacentally acquired serum lithium levels. Lithium levels in these infants decline whether they are breastfed or not, although serum levels may fall more slowly in exclusively breastfed infants. The long-term effects of lithium on infants are not certain, but limited data indicate no obvious problems in growth and development.
Lithium may be used in mothers of fullterm infants who are willing and able to monitor their infants. Because maternal lithium requirements and dosage may be increased during pregnancy, maternal serum levels should be monitored frequently postpartum and dosage reduced as necessary to avoid excessive infant exposure via breastmilk. Discontinuing lithium 24 to 48 hours before Cesarean section delivery or at the onset of spontaneous labor and resuming the prepregnancy lithium dose immediately after delivery should minimize the infant's serum lithium concentration at birth. Some investigators recommend monitoring infant serum lithium, serum creatinine, BUN, and TSH in intervals ranging from "periodic" to every 4 to 12 weeks during breastfeeding and maternal lithium therapy. One group recommends monitoring maternal and infant serum lithium at 2 and 10 days postpartum in mixed-fed infants with additional monitoring at 30 and 60 days postpartum for exclusively breastfed infants. A systematic review recommends infant lithium serum level, thyroid and renal function tests only at 10 days postpartum, then only if the infant’s serum lithium is 0.3 mEq/L or greater or if clinical signs of toxicity appear. However, others recommend close pediatric follow-up of the infant and only selective laboratory monitoring (i.e., serum lithium, TSH, BUN) if clinically indicated by unusual behavior, restlessness, feeding difficulties, sedation or abnormal growth and development. Infants who are preterm, dehydrated, or have an infection, should receive hydration and be assessed for lithium toxicity. If the infant serum lithium level is elevated, reducing the percentage of breastfeeding can decrease it.
◉ Effects in Breastfed Infants:In older reports, at least 24 infants have been reported to have been breastfed during maternal lithium therapy without any signs of toxicity or developmental problems. All were breastfed from birth and some continued to nurse for up to 6 months of maternal lithium therapy.
A 5-day-old infant developed cyanosis, lethargy, ECG T-wave inversion probably caused by lithium in breastmilk. The mother had been receiving the long-acting diuretic chlorthalidone prior to delivery which probably decreased the infant's lithium elimination and increased the neonate's lithium serum levels. Another case of probable infant lithium intoxication appeared only after the infant had a cold which may have led to dehydration and decreased lithium excretion. Two other infants had slight increases in thyrotropin (TSH) levels at 8 and 4 weeks of age, respectively, after lithium exposure that began during pregnancy. Elevated TSH continued until maternal lithium was stopped in one, and normalized by 2 months postpartum in the other, despite continued exclusive breastfeeding.
Three mothers took lithium carbonate during pregnancy and breastfeeding. The first infant was born to a mother who also took bupropion 300 mg and levothyroxine 50 to 75 mcg daily. She breastfed beyond 1 year of age. Her infant did not regain birth weight by 15 days of age, was somewhat hypotonic at 2 months of age, and was treated for gross and fine motor delay for the first year of life. The mother had a second infant on the same drug regimen. She exclusively breastfed her infant who developed normally without hypotonia. A second mother was taking a lithium dosage of 900 mg daily. Her infant gained weight slowly, but weight gain increased with breastfeeding support and she exclusively breastfed her infant for 4 months. A third mother was taking 1350 mg of lithium daily as well as escitalopram 10 mg, levothyroxine 25 mcg and heparin (dosage not stated) daily during pregnancy and breastfeeding. Her infant was normal and was exclusively breastfed until 8 weeks of age when the maternal serum lithium concentration was excessive at 2.0 mEq/L. Breastfeeding was withheld for 2 days and the dosage lowered to 600 mg daily. She then breastfed successfully until 7 months of age.
A woman with bipolar disorder took prolonged-release lithium carbonate 400 mg every 12 hours during pregnancy and postpartum. She breastfed her infant exclusively for 33 days but introduced supplements for 16 days because of slow weight gain. After the 16 days, she exclusively breastfed her infant until 2.5 months of age, when mixed feeding was begun. The infant was monitored at 17 days, 1 month, 3.5 months and 5.5 months of age. No infant side effects were observed at any time. Lithium levels were not detectable, and serum creatinine and thyroid-stimulating hormone levels were normal.
Three infants were breastfed (2 exclusive, one 50%) during maternal lithium therapy. The infants were breastfed for 5 to 21 months. All had normal growth and development, as well as normal renal and thyroid levels.
Nine infants whose mothers were taking lithium in an average dosage of 956 mg daily were exclusively breastfed for an average of 93 days (range 15 to 189 days). After routine follow-up examinations by a pediatrician, no acute growth or developmental delays were reported in any infant during the follow-up period.
Twenty-four women taking lithium during pregnancy and postpartum for bipolar disorder were divided into 3 groups: exclusive breastfeeding, partial (50 to 80%) breastfeeding, and exclusive formula feeding. Infants were followed for up to 60 days of age. During the follow-up period, pediatricians found no observable growth or developmental delay in infants in any of the three groups.
A 15-year retrospective study from two hospitals in Sweden observed 30 infants who had been breastfed by mothers taking lithium. None of the infants experienced an adverse event from lithium. All the serum sodium, potassium, creatinine, thyroid stimulating hormone and thyroid hormone (values measured were within the normal range, except for one sodium and one potassium level that were 0.1 mmol/L outside of the normal range, without any clinical consequence. No infants were described as irritable and all had normal muscle tone. About 25% of the infants had inadequate growth during their first month of life. Four mothers were advised to reduce breastfeeding and to increase the amount of formula given because of poor infant growth (n = 1), polypharmacy (n = 1) or elevated serum lithium concentrations in the infants (n = 2). Two infants were described as tired at their first outpatient visits, but their serum lithium concentration was only 0.2 mmol/L. One of them also had poor weight gain and hyperbilirubinemia at nine days of age, but one week later the baby was healthy and growing well.
◉ Effects on Lactation and Breastmilk:Lithium increases serum prolactin. Galactorrhea was reported in a woman taking lithium carbonate for 50 days. Lactation ceased with lithium discontinuation. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.
◈ What is lithium?
Lithium is a medication used to treat bipolar disorder, which is also called manic-depression. Lithium may also be used to treat other psychiatric and medical conditions. Lithium is sold under many brand names. Some brand names are: Cibalith-S®, Eskalith®, Lithane®, Lithobid® and Lithonate®.
◈ I take lithium. Can it make it harder for me to get pregnant?
Studies have not shown that taking lithium makes it more difficult for women to become pregnant.
◈ I just found out I am pregnant. Should I stop taking lithium?
Talk with your healthcare providers before making any changes to how you take this medication. Stopping lithium may cause relapse (return of symptoms), especially if it is stopped quickly. It is important that your disorder is well-controlled during pregnancy. For some people, the benefits of staying on medications that work for them during pregnancy may outweigh the potential risks. Talk with your healthcare provider about the risks and benefits of staying on lithium during pregnancy. If you continue on lithium, you should have your blood levels of lithium checked often throughout pregnancy. You may need to increase your dose during pregnancy to prevent relapse. The dose can be lowered back down before or after delivery as needed. Work with your healthcare provider to monitor and adjust doses.
◈ I am taking lithium, but would like to stop taking it before becoming pregnant. How long does the drug stay in my body?
People eliminate medications at different rates. In healthy adults, it takes up to four days, on average, for most of the lithium to be gone from the body. However, studies have shown that the longer a person has been on lithium, the longer it may take for their body to clear it completely after stopping.
◈ Does taking lithium increase the chance for miscarriage?
Miscarriage can occur in any pregnancy. Two studies have shown an increase in the chance of miscarriage with lithium use. One of the studies accounted for maternal age and history of previous miscarriage (factors that are also associated with miscarriage), but neither of the studies could account for other important factors, such as other medical conditions, body mass index, cigarette smoking, or substance use. A third study did not find an increased chance of miscarriage with lithium use. Based on the data available, it is not known if lithium increases the chance of miscarriage.
◈ Does taking lithium increase the chance of birth defects?
Every pregnancy starts out with a 3-5% chance of having a birth defect. This is called the background risk. Some studies have suggested that taking lithium in the first trimester is associated with a small increased chance of heart defects, especially a rare heart defect called Ebstein's anomaly. Ebstein's anomaly is the abnormal placement of one of the valves that controls blood flow in the heart. This rare heart defect may cause mild medical problems or a severe life-threatening condition. Other studies have not shown an association between lithium and heart defects. Based on the data available, it cannot be concluded that lithium causes birth defects. Your healthcare providers can discuss ultrasound screening options if you take lithium in pregnancy.
◈ Could taking lithium cause other pregnancy complications?
There are case reports of people developing goiters (enlarged thyroid gland in the neck) while using lithium during pregnancy. A goiter is caused by an underactive thyroid gland (called hypothyroidism). If hypothyroidism is untreated in the person who is pregnant, it can lead to a goiter in the developing baby. People who are pregnant and taking lithium should have their thyroid function monitored throughout pregnancy, so they can be treated, if needed.
◈ I need to take lithium throughout my entire pregnancy. Will it cause withdrawal symptoms in my baby after birth?
There have been case reports of decreased muscle tone, sedation (sleepiness), and trouble with breathing and feeding in the newborn when lithium was used near delivery, especially if the mother’s blood lithium level was high. Talk to your healthcare provider about whether your dose of lithium needs to be lowered before delivery. If a baby has these symptoms, the baby should fully recover in about two to ten days with treatment. Make sure your healthcare provider and your baby’s healthcare provider are aware of your lithium use, so that you and the baby can be monitored after delivery.
◈ Does taking lithium in pregnancy cause long-term problems in behavior or learning for the baby?
Studies on children up to fifteen years old who were exposed to lithium during pregnancy did not find significant physical, mental, or behavioral problems when compared to children who were not exposed to lithium during pregnancy.
◈ Can I breastfeed while taking lithium?
Continuing lithium after delivery lowers the chance of a relapse of bipolar disorder. Postpartum relapses are very serious and can lead to postpartum psychosis.Lithium passes into the breast milk and is absorbed by the baby. The amount of lithium in the nursing baby’s blood is less than what is in the breastfeeding person’s blood. If someone takes lithium while breastfeeding, they and their healthcare provider should monitor the baby for symptoms such as restlessness, low muscle tone, or trouble feeding. There are a few reports of reversible changes in the baby’s thyroid and kidney function, so monitoring the baby’s lithium level and thyroid and kidney function has been recommended. Monitoring the baby is especially important in very young or preterm infants. Be sure to talk to your healthcare provider about all your breastfeeding questions.
◈ If a male takes lithium, could it affect fertility (ability to get partner pregnant) or increase the chance of birth defects?
Some reports on lithium have found reduced sperm quality and sperm movement, while others have not. One of these reports found no reduction in fertility. Decreased sex drive was reported in another study, but this is a common side effect of depression and may not be due to the medication. There are no reports that suggest lithium use in males is associated with an increased chance of birth defects in a partner’s pregnancy. In general, exposures that fathers or sperm donors have are unlikely to increase the risks to a pregnancy. For more information, please see the MotherToBaby fact sheet Paternal Exposures at https://mothertobaby.org/fact-sheets/paternal-exposures-pregnancy/.
来源:Mother To Baby Fact Sheets
毒理性
暴露途径
该物质可以通过吸入其气溶胶和通过摄入被身体吸收。
The substance can be absorbed into the body by inhalation of its aerosol and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
Pyrazole derivatives, compositions containing such compounds and methods of use
申请人：Parmee R. Emma
公开号：US20050272794A1
公开（公告）日：2005-12-08
Pyrazoles having a naphthyl group attached are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
The present invention relates to compounds of the general formula
1
R is lower alkyl, lower alkoxy, halogen or trifluoromethyl; R
1
is halogen or hydrogen; and when p is 1, R
1
in addition to the above substituents may be taken together with R
1
to form —CH═CH—CH═CH—, R
2
and R
2′
are independently hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; and when n is 1, R
2
and R
2′
may in addition to the above substituents form —CH═CH—CH═CH—, unsubstituted or substituted by one or two substituents selected from lower alkyl or lower alkoxy; R
3
and R
3′
are hydrogen, lower alkyl or taken together with the attached carbon atom form a cycloalkyl group; R
4
is hydrogen, —N(R
5
)
2
, —N(R
5
)(CH
2
)
n
OH, —N(R
5
)S(O)
2
-lower alkyl, N(R
5
)S(O)
2
-phenyl, —N═CH—N(R
5
)
2
, —N(R
5
)C(O)R
5
;
2
3
R
5
is hydrogen, C
3-6
-cycloalkyl, benzyl or lower alkyl; R
6
is hydroxy, lower alkyl; —(CH
2
)
n
COO—(R
5
), —N(R
5
)CO-lower alkyl, hydroxy-lower alkyl;—(CH
2
)
q
CN; —(CH
2
)
n
O(CH
2
)
n
OH, —CHO or a 5-or 6 membered heterocyclic ring containing from 1 to 4 heteroatoms, selected from the group consisting of oxygen, nitrogen, and sulfur, and with one of the carbon atoms in said ring being unsubstituted or substituted with an oxo group, which heterocyclic ring is directly bonded or bonded via an alkylene group, to the remainder of the molecule;
4
is a cyclic tertiary amine which may contain one additional heteroatom selected from the group consisting of oxygen, nitrogen, and sulfur wherein any sulfur present in the ring is thio or can be oxidized to sulfoxide or sulfur dioxide, by which said cyclic tertiary amine is directly attached to the remainder of the molecule or is attached through the linker —(CH
2
)
n
N(R
5
)—; X is —C(O)N(R
5
)—, —(CH
2
)
m
O—, —(CH
2
)
m
N(R
5
)—, —N(R
5
)C(O)—, or —N(R
5
)(CH
2
)
m
—; n, p and q are 1 to 4; and m is 1 or2; and to pharmaceutically acceptable acid addition salts thereof The compounds of this invention show a high affinity to the NK-1 receptor. They may be used for the treatment of diseases relating to NK1 antagonists.
Substituted triazole derivatives as oxytocin antagonists
申请人：Brown Daniel Alan
公开号：US20060160786A1
公开（公告）日：2006-07-20
The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.
The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are CGRP receptor antagonists, useful for the treatment of migraine. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of Formulae B (after salt break) and C with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent.
Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
